Therapeutic agents useful for treating pain

ABSTRACT

A compound of formula: 
                         
wherein Ar 1 , Ar 2 , V, X, R 3 , R 4 , and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.

CONTINUING DATA

This application is a CON of Ser. No. 10/867,546 filed Jun. 14, 2004 nowU.S. Pat. No. 7,683,063, which claims the benefit of U.S. Provisionalapplication No. 60/477,744, filed Jun. 12, 2003, the disclosure of whichis incorporated by reference herein in its entirety.

1. FIELD OF THE INVENTION

The present invention relates to Cyclo(hetero)alkenyl Compounds,compositions comprising an effective amount of a Cyclo(hetero)alkenylCompound and methods for treating or preventing a condition such as paincomprising administering to an animal in need thereof an effectiveamount of a Cyclo(hetero)alkenyl Compound.

2. BACKGROUND OF THE INVENTION

Pain is the most common symptom for which patients seek medical adviceand treatment. Pain can be acute or chronic. While acute pain is usuallyself-limited, chronic pain persists for 3 months or longer and can leadto significant changes in a patient's personality, lifestyle, functionalability and overall quality of life (K. M. Foley, Pain, in CecilTextbook of Medicine 100-107 (J. C. Bennett and F. Plum eds., 20th ed.1996)).

Moreover, chronic pain can be classified as either nociceptive orneuropathic. Nociceptive pain includes tissue injury-induced pain andinflammatory pain such as that associated with arthritis. Neuropathicpain is caused by damage to the peripheral or central nervous system andis maintained by aberrant somatosensory processing. There is a largebody of evidence relating activity at both Group I metabotropicglutamate receptors (mGluR1 and mGluR5) (M. E. Fundytus, CNS Drugs15:29-58 (2001)) and vanilloid receptors (VR1) (V. Di Marzo et al.,Current Opinion in Neurobiology 12:372-379 (2002)) to pain processing.Inhibiting mGluR1 or mGluR5 reduces pain, as shown by in vivo treatmentwith antibodies selective for either mGluR1 or mGluR5, where neuropathicpain in rats was attenuated (M. E. Fundytus et al., NeuroReport9:731-735 (1998)). It has also been shown that antisense oligonucleotideknockdown of mGluR1 alleviates both neuropathic and inflammatory pain(M. E. Fundytus et al., Brit. J. Pharmacol. 132:354-367 (2001); M. E.Fundytus et al., Pharmacol., Biochem. & Behavior 73:401-410 (2002)).Small molecule antagonists for mGluR5-attenuated pain in in vivo animalmodels are disclosed in, e.g., K. Walker et al., Neuropharmacol. 40:1-9(2000) and A. Dogrul et al., Neurosci. Let. 292:115-118 (2000)).

Nociceptive pain has been traditionally managed by administeringnon-opioid analgesics, such as acetylsalicylic acid, choline magnesiumtrisalicylate, acetaminophen, ibuprofen, fenoprofen, diflusinal, andnaproxen; or opioid analgesics, including morphine, hydromorphone,methadone, levorphanol, fentanyl, oxycodone, and oxymorphone. Id. Inaddition to the above-listed treatments, neuropathic pain, which can bedifficult to treat, has also been treated with anti-epileptics (e.g.,gabapentin, carbamazepine, valproic acid, topiramate, phenytoin), NMDAantagonists (e.g., ketamine, dextromethorphan), topical lidocaine (forpost-herpetic neuralgia), and tricyclic antidepressants (e.g.,fluoxetine, sertraline and amitriptyline).

UI is uncontrollable urination, generally caused bybladder-detrusor-muscle instability. UI affects people of all ages andlevels of physical health, both in health care settings and in thecommunity at large. Physiologic bladder contraction results in largepart from acetylcholine-induced stimulation of post-ganglionicmuscarinic-receptor sites on bladder smooth muscle. Treatments for UIinclude the administration of drugs having bladder-relaxant properties,which help to control bladder-detrusor-muscle overactivity. For example,anticholinergics such as propantheline bromide and glycopyrrolate, andcombinations of smooth-muscle relaxants such as a combination of racemicoxybutynin and dicyclomine or an anticholinergic, have been used totreat UI (See, e.g., A. J. Wein, Urol. Clin. N. Am. 22:557-577 (1995);Levin et al., J. Urol. 128:396-398 (1982); Cooke et al., S. Afr. Med. J.63:3 (1983); R. K. Mirakhur et al., Anaesthesia 38:1195-1204 (1983)).These drugs are not effective, however, in all patients havinguninhibited bladder contractions.

None of the existing commercial drug treatments for UI has achievedcomplete success in all classes of UI patients, nor has treatmentoccurred without significant adverse side effects. For example,drowsiness, dry mouth, constipation, blurred vision, headaches,tachycardia, and cardiac arrhythmia, which are related to theanticholinergic activity of traditional anti-UI drugs, can occurfrequently and adversely affect patient compliance. Yet despite theprevalence of unwanted anticholinergic effects in many patients,anticholinergic drugs are currently prescribed for patients having UI.The Merck Manual of Medical Information 631-634 (R. Berkow ed., 1997).

Ulcers are sores occurring where the lining of the digestive tract hasbeen eroded by stomach acids or digestive juices. The sores aretypically well-defined round or oval lesions primarily occurring in thestomach and duodenum. About 1 in 10 people develop an ulcer. Ulcersdevelop as a result of an imbalance between acid-secretory factors, alsoknown as “aggressive factors,” such as stomach acid, pepsin, andHelicobacter pylori infection, and local mucosal-protective factors,such as secretion of bicarbonate, mucus, and prostaglandins.

Treatment of ulcers typically involves reducing or inhibiting theaggressive factors. For example, antacids such as aluminum hydroxide,magnesium hydroxide, sodium bicarbonate, and calcium bicarbonate can beused to neutralize stomach acids. Antacids, however, can causealkalosis, leading to nausea, headache, and weakness. Antacids can alsointerfere with the absorption of other drugs into the blood stream andcause diarrhea.

H₂ antagonists, such as cimetidine, ranitidine, famotidine, andnizatidine, are also used to treat ulcers. H₂ antagonists promote ulcerhealing by reducing gastric acid and digestive-enzyme secretion elicitedby histamine and other H₂ agonists in the stomach and duodenum. H₂antagonists, however, can cause breast enlargement and impotence in men,mental changes (especially in the elderly), headache, dizziness, nausea,myalgia, diarrhea, rash, and fever.

H⁺, K⁺—ATPase inhibitors such as omeprazole and lansoprazole are alsoused to treat ulcers. H⁺, K⁺—ATPase inhibitors inhibit the production ofenzymes used by the stomach to secrete acid. Side effects associatedwith H⁺, K⁺—ATPase inhibitors include nausea, diarrhea, abdominal colic,headache, dizziness, somnolence, skin rashes, and transient elevationsof plasma activities of aminotransferases.

Sucraflate is also used to treat ulcers. Sucraflate adheres toepithelial cells and is believed to form a protective coating at thebase of an ulcer to promote healing. Sucraflate, however, can causeconstipation, dry mouth, and interfere with the absorption of otherdrugs.

Antibiotics are used when Helicobacter pylori is the underlying cause ofthe ulcer. Often antibiotic therapy is coupled with the administrationof bismuth compounds such as bismuth subsalicylate and colloidal bismuthcitrate. The bismuth compounds are believed to enhance secretion ofmucous and HCO₃ ⁻, inhibit pepsin activity, and act as an antibacterialagainst H. pylori. Ingestion of bismuth compounds, however, can lead toelevated plasma concentrations of Bi⁺³ and can interfere with theabsorption of other drugs.

Prostaglandin analogues, such as misoprostal, inhibit secretion of acidand stimulate the secretion of mucous and bicarbonate and are also usedto treat ulcers, especially ulcers in patients who require nonsteroidalanti-inflammatory drugs. Effective oral doses of prostaglandinanalogues, however, can cause diarrhea and abdominal cramping. Inaddition, some prostaglandin analogues are abortifacients.

Carbenoxolone, a mineral corticoid, can also be used to treat ulcers.Carbenoxolone appears to alter the composition and quantity of mucous,thereby enhancing the mucosal barrier. Carbenoxolone, however, can leadto Na⁺ and fluid retention, hypertension, hypokalemia, and impairedglucose tolerance.

Muscarinic cholinergic antagonists such as pirenzapine and telenzapinecan also be used to reduce acid secretion and treat ulcers. Side effectsof muscarinic cholinergic antagonists include dry mouth, blurred vision,and constipation. The Merck Manual of Medical Information 496-500 (R.Berkow ed., 1997) and Goodman and Gilman's The Pharmacological Basis ofTherapeutics 901-915 (J. Hardman and L. Limbird eds., 9^(th) ed. 1996).

Inflammatory-bowel disease (“IBD”) is a chronic disorder in which thebowel becomes inflamed, often causing recurring abdominal cramps anddiarrhea. The two types of IBD are Crohn's disease and ulcerativecolitis.

Crohn's disease, which can include regional enteritis, granulomatousileitis, and ileocolitis, is a chronic inflammation of the intestinalwall. Crohn's disease occurs equally in both sexes and is more common inJews of eastern-European ancestry. Most cases of Crohn's disease beginbefore age 30 and the majority start between the ages of 14 and 24. Thedisease typically affects the full thickness of the intestinal wall.Generally the disease affects the lowest portion of the small intestine(ileum) and the large intestine, but can occur in any part of thedigestive tract.

Early symptoms of Crohn's disease are chronic diarrhea, crampy abdominalpain, fever, loss of appetite, and weight loss. Complications associatedwith Crohn's disease include the development of intestinal obstructions,abnormal connecting channels (fistulas), and abscesses. The risk ofcancer of the large intestine is increased in people who have Crohn'sdisease. Often Crohn's disease is associated with other disorders suchas gallstones, inadequate absorption of nutrients, amyloidosis,arthritis, episcleritis, aphthous stomatitis, erythema nodosum, pyodermagangrenosum, ankylosing spondylitis, sacroilitis, uveitis, and primarysclerosing cholangitis. There is no known cure for Crohn's disease.

Cramps and diarrhea, side effects associated with Crohn's disease, canbe relieved by anticholinergic drugs, diphenoxylate, loperamide,deodorized opium tincture, or codeine. Generally, the drug is takenorally before a meal.

Broad-spectrum antibiotics are often administered to treat the symptomsof Crohn's disease. The antibiotic metronidazole is often administeredwhen the disease affects the large intestine or causes abscesses andfistulas around the anus. Long-term use of metronidazole, however, candamage nerves, resulting in pins-and-needles sensations in the arms andlegs. Sulfasalazine and chemically related drugs can suppress mildinflammation, especially in the large intestine. These drugs, however,are less effective in sudden, severe flare-ups. Corticosteroids, such asprednisone, reduce fever and diarrhea and relieve abdominal pain andtenderness. Long-term corticosteroid therapy, however, invariablyresults in serious side effects such as high blood-sugar levels,increased risk of infection, osteoporosis, water retention, andfragility of the skin. Drugs such as azathioprine and mercaptourine cancompromise the immune system and are often effective for Crohn's diseasein patients that do not respond to other drugs. These drugs, however,usually need 3 to 6 months before they produce benefits and can causeserious side effects such as allergy, pancreatitis, and lowwhite-blood-cell count.

When Crohn's disease causes the intestine to be obstructed or whenabscesses or fistulas do not heal, surgery can be necessary to removediseased sections of the intestine. Surgery, however, does not cure thedisease, and inflammation tends to recur where the intestine isrejoined. In almost half of the cases a second operation is needed. TheMerck Manual of Medical Information 528-530 (R. Berkow ed., 1997).

Ulcerative colitis is a chronic disease in which the large intestinebecomes inflamed and ulcerated, leading to episodes of bloody diarrhea,abdominal cramps, and fever. Ulcerative colitis usually begins betweenages 15 and 30; however, a small group of people have their first attackbetween ages 50 and 70. Unlike Crohn's disease, ulcerative colitis neveraffects the small intestine and does not affect the full thickness ofthe intestine The disease usually begins in the rectum and the sigmoidcolon and eventually spreads partially or completely throughout thelarge intestine. The cause of ulcerative colitis is unknown.

Treatment of ulcerative colitis is directed to controlling inflammation,reducing symptoms, and replacing lost fluids and nutrients.Anticholinergic drugs and low doses of diphenoxylate or loperamide areadministered for treating mild diarrhea. For more intense diarrheahigher doses of diphenoxylate or loperamide, or deodorized opiumtincture or codeine are administered. Sulfasalazine, olsalazine,prednisone, or mesalamine can be used to reduce inflammation.Azathioprine and mercaptopurine have been used to maintain remissions inulcerative-colitis patients who would otherwise need long-termcorticosteroid treatment. In severe cases of ulcerative colitis thepatient is hospitalized and given corticosteroids intravenously. Peoplewith severe rectal bleeding can require transfusions and intravenousfluids. If toxic colitis develops and treatments fail, surgery to removethe large intestine can be necessary. Non-emergency surgery can beperformed if cancer is diagnosed, precancerous lesions are detected, orunremitting chronic disease would otherwise make the person an invalidor dependent on high doses of corticosteroids. Complete removal of thelarge intestine and rectum permanently cures ulcerative colitis. TheMerck Manual of Medical Information 530-532 (R. Berkow ed., 1997) andGoodman and Gilman's The Pharmacological Basis of Therapeutics (J.Hardman and L. Limbird eds., 9^(th) ed. 1996).

Irritable-bowel syndrome (“IBS”) is a disorder of motility of the entiregastrointestinal tract, causing abdominal pain, constipation, and/ordiarrhea. IBS affects three-times more women than men. In IBS stimulisuch as stress, diet, drugs, hormones, or irritants can cause thegastrointestinal tract to contract abnormally. During an episode of IBS,contractions of the gastrointestinal tract become stronger and morefrequent, resulting in the rapid transit of food and feces through thesmall intestine, often leading to diarrhea. Cramps result from thestrong contractions of the large intestine and increased sensitivity ofpain receptors in the large intestine.

There are two major types of IBS. The first type, spastic-colon type, iscommonly triggered by eating, and usually produces periodic constipationand diarrhea with pain. Mucous often appears in the stool. The pain cancome in bouts of continuous dull aching pain or cramps, usually in thelower abdomen. The person suffering from spastic-colon type MS can alsoexperience bloating, gas, nausea, headache, fatigue, depression,anxiety, and difficulty concentrating. The second type of IBS usuallyproduces painless diarrhea or constipation. The diarrhea can beginsuddenly and with extreme urgency. Often the diarrhea occurs soon aftera meal and can sometimes occur immediately upon awakening.

Treatment of IBS typically involves modification of an IBS-patient'sdiet. Often it is recommended that an IBS patient avoid beans, cabbage,sorbitol, and fructose. A low-fat, high-fiber diet can also help someIBS patients. Regular physical activity can also help keep thegastrointestinal tract functioning properly. Drugs such as propanthelinethat slow the function of the gastrointestinal tract are generally noteffective for treating IBS. Antidiarrheal drugs, such as diphenoxylateand loperamide, help with diarrhea. The Merck Manual of MedicalInformation 525-526 (R. Berkow ed., 1997).

Certain pharmaceutical agents have been administered for treatingaddiction. U.S. Pat. No. 5,556,838 to Mayer et al. discloses the use ofnontoxic NMDA-blocking agents co-administered with an addictivesubstance to prevent the development of tolerance or withdrawalsymptoms. U.S. Pat. No. 5,574,052 to Rose et al. disclosesco-administration of an addictive substance with an antagonist topartially block the pharmacological effects of the addictive substance.U.S. Pat. No. 5,075,341 to Mendelson et al. discloses the use of a mixedopiate agonist/antagonist to treat cocaine and opiate addiction. U.S.Pat. No. 5,232,934 to Downs discloses administration of3-phenoxypyridine to treat addiction. U.S. Pat. Nos. 5,039,680 and5,198,459 to Imperato et al. disclose using a serotonin antagonist totreat chemical addiction. U.S. Pat. No. 5,556,837 to Nestler et. al.discloses infusing BDNF or NT-4 growth factors to inhibit or reverseneurological adaptive changes that correlate with behavioral changes inan addicted individual. U.S. Pat. No. 5,762,925 to Sagan disclosesimplanting encapsulated adrenal medullary cells into an animal's centralnervous system to inhibit the development of opioid tolerance. U.S. Pat.No. 6,204,284 to Beer et al. discloses racemic(±)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane for use in theprevention or relief of a withdrawal syndrome resulting from addictionto drugs and for the treatment of chemical dependencies.

Without treatment, Parkinson's disease progresses to a rigid akineticstate in which patients are incapable of caring for themselves. Deathfrequently results from complications of immobility, includingaspiration pneumonia or pulmonary embolism. Drugs commonly used for thetreatment of Parkinson's disease include carbidopa/levodopa, pergolide,bromocriptine, selegiline, amantadine, and trihexyphenidylhydrochloride. There remains, however, a need for drugs useful for thetreatment of Parkinson's disease and having an improved therapeuticprofile.

Currently, benzodiazepines are the most commonly used anti-anxietyagents for generalized anxiety disorder. Benzodiazepines, however, carrythe risk of producing impairment of cognition and skilled motorfunctions, particularly in the elderly, which can result in confusion,delerium, and falls with fractures. Sedatives are also commonlyprescribed for treating anxiety. The azapirones, such as buspirone, arealso used to treat moderate anxiety. The azapirones, however, are lessuseful for treating severe anxiety accompanied with panic attacks.

Examples of drugs for treating a seizure and epilepsy includecarbamazepine, ethosuximide, gabapentin, lamotrigine, phenobarbital,phenytoin, primidone, valproic acid, trimethadione, benzodiazepines,γ-vinyl GABA, acetazolamide, and felbamate. Anti-seizure drugs, however,can have side effects such as drowsiness; hyperactivity; hallucinations;inability to concentrate; central and peripheral nervous systemtoxicity, such as nystagmus, ataxia, diplopia, and vertigo; gingivalhyperplasia; gastrointestinal disturbances such as nausea, vomiting,epigastric pain, and anorexia; endocrine effects such as inhibition ofantidiuretic hormone, hyperglycemia, glycosuria, osteomalacia; andhypersensitivity such as scarlatiniform rash, morbilliform rash,Stevens-Johnson syndrome, systemic lupus erythematosus, and hepaticnecrosis; and hematological reactions such as red-cell aplasia,agranulocytosis, thrombocytopenia, aplastic anemia, and megaloblasticanemia. The Merck Manual of Medical Information 345-350 (R. Berkow ed.,1997).

Symptoms of strokes vary depending on what part of the brain isaffected. Symptoms include loss or abnormal sensations in an arm or legor one side of the body, weakness or paralysis of an arm or leg or oneside of the body, partial loss of vison or hearing, double vision,dizziness, slurred speech, difficulty in thinking of the appropriateword or saying it, inability to recognize parts of the body, unusualmovements, loss of bladder control, imbalance, and falling, andfainting. The symptoms can be permanent and can be associated with comaor stupor. Examples of drugs for treating strokes include anticoagulantssuch as heparin, drugs that break up clots such as streptokinase ortissue plasminogen activator, and drugs that reduce swelling such asmannitol or corticosteroids. The Merck Manual of Medical Information352-355 (R. Berkow ed., 1997).

Pruritus is an unpleasant sensation that prompts scratching.Conventionally, pruritus is treated by phototherapy with ultraviolet Bor PUVA or with therapeutic agents such as naltrexone, nalmefene,danazol, tricyclics, and antidepressants.

Selective antagonists of the metabotropic glutamate receptor 5(“mGluR5”) have been shown to exert analgesic activity in in vivo animalmodels (K. Walker et al., Neuropharmacol. 40:1-9 (2000) and A. Dogrul etal., Neurosci. Let. 292(2):115-118 (2000)).

Selective antagonists of the mGluR5 receptor have also been shown toexert anxiolytic and anti-depressant activity in in vivo animal models(E. Tatarczynska et al., Brit. J. Pharmacol. 132(7):1423-1430 (2001) andP. J. M. Will et al., Trends in Pharmacological Sci. 22(7):331-37(2001)).

Selective antagonists of the mGluR5 receptor have also been shown toexert anti-Parkinson activity in vivo (K. J. Ossowska et al.,Neuropharmacol. 41(4):413-20 (2001) and P. J. M. Will et al., Trends inPharmacological Sci. 22(7):331-37 (2001)).

Selective antagonists of the mGluR5 receptor have also been shown toexert anti-dependence activity in vivo (C. Chiamulera et al., NatureNeurosci. 4(9):873-74 (2001)).

U.S. published patent application no. US 2002/0091116 to Zhu et al.describes a class of compounds useful as selective inhibitors ofisolated factor Xa or useful when assembled in the prothrombinasecomplex.

U.S. Pat. No. 5,474,996 to Caille et al. describes a class of pyrimidinederivatives having angiotensin II inhibiting activity.

U.S. Pat. No. 6,063,930 to Dinsmore et al. describes a class ofcompounds that are useful for inhibiting farnesyl-protein transferaseand for the farnesylation of Ras, an oncogene protein.

Citation of any reference in Section 2 of this application is not to beconstrued as an admission that such reference is prior art to thepresent application.

3. SUMMARY OF THE INVENTION

The present invention encompasses compounds of formula:

and pharmaceutically acceptable salts thereof, wherein

Ar¹ is

Ar² is

V is N or CH;

X is O or S;

R₁ is —H, -halo, —(C₁-C₄)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo);

each R₂ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to        10-membered)heteroaryl, each of which is unsubstituted or        substituted with one or more R₆ groups;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

R₄ is —H or —(C₁-C₆)alkyl;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each R₈ is independently —(C₁-C₁₀)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇, —R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇,—R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂,—(C₁-C₁₀)alkyl, or -(3- to 7-membered)heterocycle;

each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl;

each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇;

Y₁ and Y₂ are —CH₂— and —CH₂—, —O— and —O—, —NH— and —NH—, —S— and —S—,CH₂— and —O—, —CH₂— and —NH—, —CH₂— and —S—, —O— and —CH₂—, —NH— and—CH₂—, —S— and —CH₂—, and —CH₂—, —O— and —NH—, —NH— and —O—, —S— and—NH—, or —NH— and —S— respectively;

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

n is an integer ranging from 0 to 3;

p is an integer ranging from 0 to 2;

q is an integer ranging from 0 to 6;

r is an integer ranging from 0 to 5; and

s is an integer ranging from 0 to 4.

The present invention encompasses compounds of formula:

and pharmaceutically acceptable salts thereof, wherein

Ar¹ is

Ar² is

V is N or CH;

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo);

each R₂ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to        10-membered)heteroaryl, each of which is unsubstituted or        substituted with one or more R₆ groups;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂ (halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇;

each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇;

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

n is an integer ranging from 0 to 3;

p is an integer ranging from 0 to 2;

q is an integer ranging from 0 to 6;

r is an integer ranging from 0 to 5; and

s is an integer ranging from 0 to 4.

A Compound of Formula (I) or (IA) or a pharmaceutically acceptable saltthereof (a “Cyclo(hetero)alkenyl Compound”), is useful for treating orpreventing pain, UI, an ulcer, IBD, IBS, an addictive disorder,Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure,a pruritic condition, psychosis, a cognitive disorder, a memory deficit,restricted brain function, Huntington's chorea, ALS, dementia,retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, ordepression (each being a “Condition”) in an animal.

The invention also relates to compositions comprising an effectiveamount of a Cyclo(hetero)alkenyl Compound and a pharmaceuticallyacceptable carrier or excipient. The compositions are useful fortreating or preventing a Condition in an animal.

The invention further relates to methods for treating a Condition,comprising administering to an animal in need thereof an effectiveamount of a Cyclo(hetero)alkenyl Compound.

The invention further relates to methods for preventing a Condition,comprising administering to an animal in need thereof an effectiveamount of a Cyclo(hetero)alkenyl Compound.

The invention still further relates to methods for inhibiting VanilloidReceptor 1 (“VR1”) function in a cell, comprising contacting a cellcapable of expressing VR1 with an effective amount of aCyclo(hetero)alkenyl Compound.

The invention still further relates to a method for preparing acomposition, comprising the step of admixing a Cyclo(hetero)alkenylCompound and a pharmaceutically acceptable carrier or excipient.

The invention still further relates to a kit comprising a containercontaining an effective amount of a Cyclo(hetero)alkenyl Compound. Thekit may further comprise printed instructions for using theCyclo(hetero)alkenyl Compound to treat any of the aforementionedConditions.

The present invention can be understood more fully by reference to thefollowing detailed description and illustrative examples, which areintended to exemplify non-limiting embodiments of the invention.

4. DETAILED DESCRIPTION OF THE INVENTION 4.1 Cyclo(Hetero)AlkenylCompounds 4.1.1 Cyclo(Hetero)Alkenyl Compounds of Formula (I)

The present invention encompasses Compounds of Formula (I)

and pharmaceutically acceptable salts thereof, where V, X, Ar¹, Ar², R₃,R₄, and m are defined above for the Cyclo(hetero)alkenyl Compounds ofFormula (I).

In one embodiment, each R₈ is independently —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇,—R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇, —R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇,—C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂, —CH(C(halo)₃)₂,—CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃, —OC(halo)₂CH(halo)₂,—OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂, —(C₁-C₁₀)alkyl, or-(3- to 7-membered)heterocycle.

In another embodiment, R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃,—NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, Ar² is

In another embodiment, Ar¹ is

In another embodiment, Ar² is

and Ar¹ is

In another embodiment, each R₈ is independently —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.

In another embodiment, Ar² is

and each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇.

In another embodiment, Ar¹ is

and each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇.

In another embodiment, Ar² is

and each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇.

In another embodiment, R₄ is —H.

In another embodiment, Ar² is

and R₄ is —H.

In another embodiment, Ar¹ is

and R₄ is —H.

In another embodiment, Ar² is

Ar¹ is

and R₄ is —H.

In another embodiment, R₄ is —H and each R₈ is independently—(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.

In another embodiment, Ar² is

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇, and

R₄ is —H.

In another embodiment, Ar¹ is

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂ (halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇, and

R₄ is —H.

In another embodiment, Ar¹ is

Ar¹ is

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂ (halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇, and R₄ is —H.

In another embodiment, R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃,—NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo); and Ar² is

In another embodiment, Ar¹ is

and R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo).

In another embodiment, Ar² is

Ar¹ is

and R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo).

In another embodiment, R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃,—NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo); and each R₈ is independently—(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.

In another embodiment, Ar² is

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂ (halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇; and R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃,—NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo); and each R₈ is independently —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.

In another embodiment, Ar² is

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂ (halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or S(O)₂R₇; Ar¹ is

and R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo).

In another embodiment, R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃,—NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo); and R₄ is —H.

In another embodiment, Ar² is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo); and R₄ is —H.

In another embodiment, Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo); and R₄ is —H.

In another embodiment, Ar² is

Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo); and R₄ is —H.

In another embodiment, R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃,—NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo); R₄ is —H; and each R₈ isindependently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl,—(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇,—NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or—S(O)₂R₇.

In another embodiment, Ar² is

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂ (halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇; R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃,—NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo); and R₄ is —H.

In another embodiment, Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃,—CH(halo)₂, or —CH₂(halo); each R₈ is independently —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇, and R₄ is —H.

In another embodiment, Ar² is

each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)₂R₇; Ar¹ is

and R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, C(halo)₃, —CH(halo)₂,or —CH₂(halo).

In one embodiment, Ar¹ is a pyridyl group.

In another embodiment, Ar¹ is a pyrimidyl group

In another embodiment, Ar¹ is a pyrazinyl group.

In another embodiment, Ar¹ is a pyridazinyl group.

In another embodiment, Ar¹ is a thiadiazolyl group.

In another embodiment, Ar¹ is

In another embodiment, Ar¹ is

In another embodiment, Ar¹ is

In another embodiment, V is N.

In another embodiment, V is CH.

In another embodiment, Ar² is a benzoimidazolyl group.

In another embodiment, Ar² is a benzothiazolyl group.

In another embodiment, Ar² is a benzooxazolyl group.

In another embodiment, Ar² is a 5-benzodioxolyl group, a5-benzodithiolyl group, a 5-dihydroindenyl group, a5-dihydrobenzoimidazolyl group, a 6-dihydrobenzofuranyl group, a5-dihydrobenzofuranyl group, a 6-indolinyl group, a 5-indolinyl group, a6-dihydrobenzothiopheneyl group, a 5-dihydrobenzothiopheneyl group, a5-dihydrobenzooxazolyl group, a 6-dihydrobenzooxazolyl group, a5-dihydrobenzothiazolyl group, or a 6-dihydrobenzothiazolyl group.

In another embodiment, Ar² is a 5-benzodioxolyl group, a5-benzodithiolyl group, a 5-dihydroindenyl group, a5-dihydrobenzoimidazolyl group, a 6-dihydrobenzofuranyl group, a5-dihydrobenzofuranyl group, a 6-indolinyl group, a 5-indolinyl group, a6-dihydrobenzothiopheneyl group, or a 5-dihydrobenzothiopheneyl group.

In another embodiment, Ar² is a 5-dihydroindenyl group, a5-dihydrobenzoimidazolyl group, a 5-benzodioxolyl group, or a5-benzodithiolyl group.

In another embodiment, Ar² is a 5-benzodioxolyl group or a5-benzodithiolyl group.

In another embodiment, Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar² is a 5-benzodithiolyl group.

In another embodiment, Ar² is

In another embodiment, Ar² is

In another embodiment, Ar² is

In another embodiment, Ar² is

In another embodiment, Ar² is

In another embodiment, Ar² is

In another embodiment, p or n is 0.

In another embodiment, p or n is 1.

In another embodiment, m is 0.

In another embodiment, m is 0 and V is N.

In another embodiment, m is 0 and V is CH.

In another embodiment, m is 1.

In another embodiment, m is 1 and V is N.

In another embodiment, m is 1 and V is CH.

In another embodiment, Ar² is

and s is 0.

In another embodiment, Ar² is

and s is 1.

In another embodiment, Ar² is

and q is 0.

In another embodiment, Ar² is

and q is 1.

In another embodiment, Ar² is

and r is 0.

In another embodiment, Ar² is

and r is 0.

In another embodiment, Ar² is a benzothiazolyl group and s is 0.

In another embodiment, Ar² is a benzoimidazolyl group and s is 0.

In another embodiment, Ar² is a benzooxazolyl group and s is 0.

In another embodiment, Ar² is a benzothiazolyl group and s is 1.

In another embodiment, Ar² is a benzoimidazolyl group and s is 1.

In another embodiment, Ar² is a benzooxazolyl group and s is 1.

In another embodiment, Ar² is a 5-benzodioxolyl group and each R₉ is —H.

In another embodiment, Ar² is a 5-benzodioxolyl group and each R₉ is —F.

In another embodiment, R₁ is —H.

In another embodiment, R₁ is -halo.

In another embodiment, R₁ is —(C₁-C₄)alkyl.

In another embodiment, R₁ is —CH₃ or —CH₂CH₃.

In another embodiment, R₁ is —CH₂CH₃.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, n or p is 1 and R₂ is -halo, —CN, —OH, —NO₂, or—NH₂.

In another embodiment, n or p is 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, n or p is 1 and R₂ is -phenyl, -naphthyl,—(C₁₄)aryl or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups.

In another embodiment, m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring, and R₃ is -halo, —CN, —OH,—NO₂, or —NH₂;

In another embodiment, m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring, and R₃ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring, and R₃ is -phenyl,-naphthyl, —(C₁₄)aryl or -(5- to 10-membered)heteroaryl, each of whichis unsubstituted or substituted with one or more R₆ groups.

In another embodiment, m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring, and R₃ is —CH₃.

In another embodiment, R₄ is —H.

In another embodiment, R₄ is —(C₁-C₆)alkyl.

In another embodiment, R₄ is ethyl.

In another embodiment, R₄ is methyl.

In another embodiment, R₄ is —H or methyl.

In another embodiment, each R₈ is independently —(C₁-C₁₀)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -(3- to 7-membered)heterocycle, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —R₇C(O)OR₇, —OC(O)R₇,—R₇OC(O)R₇, —OC(O)OR₇, —R₇OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.

In another embodiment, each R₈ is independently —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, —S(O)₂R₇, or —C(halo)₂C(halo)₃.

In another embodiment, Ar² is a benzothiazolyl group, benzoimidazolylgroup, or benzooxazolyl group and each R₈ is independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, Ar² is

and each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), or—C(OH)(CF₃)₂.

In another embodiment, Ar² is

and each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), or—C(OH)(CF₃)₂.

In another embodiment, Ar² is

and each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), or—C(OH)(CF₃)₂.

In another embodiment, Ar² is

and each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇.

In another embodiment, Ar¹ is a pyridyl group; V is N; m is 0, and Ar²is a benzothiazolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; R₈ s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group;and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; and s is 1. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; —F—Br, or —I; Ar² is a benzothiazolyl group; s is1; and R₈ is —F. In another embodiment, the R₃ group is attached to 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzothiazolyl group; s is1; and R₈ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a benzothiazolyl group; sis 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —CF₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group, V is CH; m is 0, and Ar²is a benzothiazolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; R₈ s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is a benzothiazolyl group; s is 1; and R₈is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; s is 1; and R₈is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group;and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; and s is 1. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzothiazolyl group; s is1; and R₈ is —F. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzothiazolyl group; s is1; and R₈ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a benzothiazolyl group; sis 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —CF₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzothiazolyl group; sis 1; and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzothiazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group, V is N; m is 0, and Ar²is a benzoimidazolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Br, or —I; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; R₈ s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; s is 1; and R₈is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is a benzoimidazolyl group; s is 1; andR₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group;and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 5- or 6-position ofthe cyclo(hetero)alkenyl ring and the carbon atom to which the R₃ groupis attached has the (R) configuration. In another embodiment, the R₃group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; and s is 1. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -halo. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -halo. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; s is1; and R₈ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a benzoimidazolyl group; sis 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —CF₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —CF₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -tert-butyl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -tert-butyl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group, V is CH; m is 0, and Ar²is a benzoimidazolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; R₈ s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; s is 1; and R₈is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is a benzoimidazolyl group; s is 1; andR₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; s is 1; andR₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group;and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; and s is 1. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -halo. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -halo. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzoimidazolyl group; s is1; and R₈ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a benzoimidazolyl group; sis 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —CF₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —CF₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —CF₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is —OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzoimidazolyl group; sis 1; and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzoimidazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -tert-butyl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzoimidazolyl group; s is 1; and R₈is -tert-butyl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group, V is N; m is 0, and Ar²is a benzooxazolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; R₈ s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is a benzooxazolyl group; s is 1; and R₈is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; ands is 0. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; and s is 1. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is1; and R₈ is —F. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is1; and R₈ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a benzooxazolyl group; sis 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —CF₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group, V is CH; m is 0, and Ar²is a benzooxazolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; R₈ s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group s is 1; and R₈ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is a benzooxazolyl group; s is 1; and R₈is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —CF₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; s is 1; and R₈is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is —OCH₂CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; R₈ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; ands is 0. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; and s is 0. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; and s is 1. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (R) configuration. In another embodiment, theR₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is1; and R₈ is —F. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a benzooxazolyl group; s is1; and R₈ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a benzooxazolyl group; sis 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-positioncyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —CF₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—CF₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is—OCH₂CH₃. In another embodiment, the R₃ group is attached to the 3-, 5-or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a benzooxazolyl group; sis 1; and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a benzooxazolyl group; s is 1; and R₈ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, V is N, Ar¹ is a pyridyl group, m is 0, and Ar²is

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Br, or —I; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar¹ is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F —Br, or —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F —Br, or —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is chloro. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃, Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃, Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is

r is 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH3; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃ Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, V is CH, Ar¹ is a pyridyl group, m is 0, and Ar²is

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

and r is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —F. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is chloro. In another embodiment, R₈ is at the 4-positionof the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —I. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 4-position ofthe phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -tent-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

and r is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar¹ is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is

r is 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is —OCH₂CH₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

r is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the4-position of the phenyl ring.

In another embodiment, V is N, Ar¹ is a pyridyl group, m is 0, and Ar²is

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F —Br, or —I; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F —Br, or —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is chloro. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃, Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃, Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is

s is 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH3; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, V is CH, Ar¹ is a pyridyl group, m is 0, and Ar²is

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

and s is 0.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃;

Ar² is

s is 1 and R₈ is -halo. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar¹ is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —Br. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; AR² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —F. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F—Br, or —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is chloro. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —I. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, R₈ is at the 5-position ofthe Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, R₈ is at the 5-positionof the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl —Br, or —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

and s is 0. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, R₈ is at the 5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to R₃ group is attachedhas the (S) configuration. In yet another embodiment, the R₃ group isattached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is -halo. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —F. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —Cl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is

s is 1; and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring. In another embodiment, R₈ is at the 5-position of the Ar² pyridylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CF₃. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is —CH₂CF₃. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is

s is 1 and R₈ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring. In another embodiment, R₈ is at the5-position of the Ar² pyridyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; m is 0, and Ar²is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F, —Cl; —Br, or —I; Ar² is a 5-benzodioxolyl group; R₉ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; and Ar² is a 5-benzodioxolylgroup. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is -halo. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; —F—Br, or —I; Ar² is a 5-benzodioxolyl group; andeach R₉ is —F. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a 5-benzodioxolyl group; andeach R₉ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a 5-benzodioxolyl group;and each R₉ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is -ethyl. In another embodiment, the R₃ group is attachedto the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and thecarbon atom to which the R₃ group is attached has the (R) configuration.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (S) configuration. In yet anotherembodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is -isopropyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is N; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group, V is CH; m is 0, and Ar²is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -halo.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —Br.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F—Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group and each R₉ is —Cl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl, —F, —Br, or —I, Ar² is a 5-benzodioxolyl group; and each R₉is —I.

in another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; and Ar² is a 5-benzodioxolyl group.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is —CH₃.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -ethyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; and each R₉is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -isopropyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; each R₉ is-tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 0;R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is -tert-butyl.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; and Ar² is a 5-benzodioxolylgroup. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; and Ar² is a 5-benzodioxolyl group. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (R) configuration. In another embodiment, the R₃ groupis attached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (S)configuration. In yet another embodiment, the R₃ group is attached tothe 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is -halo. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-halo. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is —Br. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Br. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a 5-benzodioxolyl group; andeach R₉ is —F. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —F.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—F. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is CH₃; R₁ is —Cl, —F—Br, or —I; Ar² is a 5-benzodioxolyl group; andeach R₉ is —Cl. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—Cl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)(alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl, —F, —Br, or —I, Ar² is a 5-benzodioxolyl group;and each R₉ is —I. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is —I.In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—I. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is —CH₃. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is—CH₃. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring. Inanother embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1; R₃is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group; andeach R₉ is -ethyl. In another embodiment, the R₃ group is attached tothe 3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (R) configuration. Inanother embodiment, the R₃ group is attached to the 3-, 5- or 6-positionof the cyclo(hetero)alkenyl ring and the carbon atom to which the R₃group is attached has the (S) configuration. In yet another embodiment,the R₃ group is attached to the 2-position of the cyclo(hetero)alkenylring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-ethyl. In another embodiment, the R₃ group is attached to the 3-, 5- or6-position of the cyclo(hetero)alkenyl ring and the carbon atom to whichthe R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is -isopropyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-isopropyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F, —Cl, —Br, or —I; Ar² is a 5-benzodioxolyl group;and each R₉ is -tert-butyl. In another embodiment, the R₃ group isattached to the 3-, 5- or 6-position of the cyclo(hetero)alkenyl ringand the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, the R₃ group is attached to the3-, 5- or 6-position of the cyclo(hetero)alkenyl ring and the carbonatom to which the R₃ group is attached has the (S) configuration. In yetanother embodiment, the R₃ group is attached to the 2-position of thecyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —F; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Cl; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —Br; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —I; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CH₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In another embodiment, Ar¹ is a pyridyl group; V is CH; n is 0; m is 1;R₃ is —CH₃; R₁ is —CF₃; Ar² is a 5-benzodioxolyl group; and each R₉ is-tert-butyl. In another embodiment, the R₃ group is attached to the 3-,5- or 6-position of the cyclo(hetero)alkenyl ring and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the R₃ group is attached to the 3-, 5- or 6-position of thecyclo(hetero)alkenyl ring and the carbon atom to which the R₃ group isattached has the (S) configuration. In yet another embodiment, the R₃group is attached to the 2-position of the cyclo(hetero)alkenyl ring.

In the Cyclo(hetero)alkenyl Compounds that have an R₃ group, the R₃group can be attached to the carbon at the 2-, 3-, 5- or 6-position ofthe cyclo(hetero)alkenyl ring. In one embodiment, the R₃ group isattached to the carbon at the 3-position of the cyclo(hetero)alkenylring. In another embodiment, the R₃ group is attached to the carbon atthe 5-position of the cyclo(hetero)alkenyl ring. In another embodiment,the R₃ group is attached to the carbon at the 6-position of thecyclo(hetero)alkenyl ring. In another embodiment, the R₃ group isattached to the carbon at the 2-position of the cyclo(hetero)alkenylring.

In one embodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group;the carbon atom to which the R₃ group is attached is at the 3-, 5- or6-position of the tetrahydropiperidine ring; and the carbon atom towhich the R₃ group is attached has the (R) configuration. In anotherembodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group; thecarbon atom to which the R₃ group is attached is at the 3-, 5- or6-position of the tetrahydropiperidine ring; and the carbon atom towhich the R₃ group is attached has the (S) configuration.

In another embodiment, the Cyclo(hetero)alkenyl Compound has an R₃group, the R₃ group is attached to the carbon that is at the 3-positionof the tetrahydropiperidine ring, and the carbon to which the R₃ groupis attached is in the (R) configuration. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon that is at the 3-position of the tetrahydropiperidinering, the carbon to which the R₃ group is attached is in the (R)configuration, and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted withone or more halo groups. In another embodiment, the Cyclo(hetero)alkenylCompound has an R₃ group, the R₃ group is attached to the carbon that isat the 3-position of the tetrahydropiperidine ring, the carbon to whichthe R₃ group is attached is in the (R) configuration, and R₃ is —CH₃. Inanother embodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group,the R₃ group is attached to the carbon that is at the 3-position of thetetrahydropiperidine ring, the carbon to which the R₃ group is attachedis in the (R) configuration, and R₃ is —CF₃. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon that is at the 3-position of the tetrahydropiperidinering, the carbon to which the R₃ group is attached is in the (R)configuration, and R₃ is —CH₂CH₃.

In another embodiment, the Cyclo(hetero)alkenyl Compound has an R₃group, the R₃ group is attached to the carbon atom at the 6-position ofthe tetrahydropiperidine ring, and the carbon to which the R₃ group isattached is in the (R) configuration. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 6-position of the tetrahydropiperidine ring,the carbon to which the R₃ group is attached is in the (R)configuration, and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted withone or more halo groups. In another embodiment, the Cyclo(hetero)alkenylCompound has an R₃ group, the R₃ group is attached to the carbon atom atthe of the tetrahydropiperidine ring, the carbon to which the R₃ groupis attached is in the (R) configuration, and R₃ is —CH₃. In anotherembodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group, the R₃group is attached to the carbon atom at the 6-position of thetetrahydropiperidine ring, the carbon to which the R₃ group is attachedis in the (R) configuration, and R₃ is —CF₃. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 6-position of the tetrahydropiperidine ring,the carbon to which the R₃ group is attached is in the (R)configuration, and R₃ is —CH₂CH₃.

In another embodiment, the Cyclo(hetero)alkenyl Compound has an R₃group, the R₃ group is attached to the carbon atom at the 5-position ofthe tetrahydropiperidine ring, and the carbon to which the R₃ group isattached is in the (R) configuration. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 5-position of the tetrahydorpiperidine ring,the carbon to which the R₃ group is attached is in the (R)configuration, and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted withone or more halo groups. In another embodiment, the Cyclo(hetero)alkenylCompound has an R₃ group, the R₃ group is attached to the carbon atom atthe 5-position of the tetrahydropiperidine ring, the carbon to which theR₃ group is attached is in the (R) configuration, and R₃ is —CH₃. Inanother embodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group,the R₃ group is attached to the carbon atom at the 5-position of thetetrahydropiperidine ring, the carbon to which the R₃ group is attachedis in the (R) configuration, and R₃ is —CF₃. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 5-position of the tetrahydropiperidine ring.The R₃ group is in the (R) configuration, and R₃ is —CH₂CH₃.

In another embodiment, the Cyclo(hetero)alkenyl Compound has an R₃group, the R₃ group is attached to the carbon that is at the 3-positionof the tetrahydropiperidine ring, and the carbon to which the R₃ groupis attached is in the (S) configuration. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon that is at the 3-position of the tetrahydropiperidinering, the carbon to which the R₃ group is attached is in the (S)configuration, and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted withone or more halo groups. In another embodiment, the Cyclo(hetero)alkenylCompound has an R₃ group, the R₃ group is attached to the carbon that isat the 3-position of the tetrahydropiperidine ring, the carbon to whichthe R₃ group is attached is in the (S) configuration, and R₃ is —CH₃. Inanother embodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group,the R₃ group is attached to the carbon that is at the 3-position of thetetrahydropiperidine ring, the carbon to which the R₃ group is attachedis in the (S) configuration, and R₃ is —CF₃. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon that is at the 3-position of the tetrahydropiperidinering, the carbon to which the R₃ group is attached is in the (S)configuration, and R₃ is —CH₂CH₃.

In another embodiment, the Cyclo(hetero)alkenyl Compound has an R₃group, the R₃ group is attached to the carbon atom at the 6-position ofthe tetrahydropiperidine ring, and the carbon to which the R₃ group isattached is in the (S) configuration. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 6-position of the tetrahydropiperidine ring,the carbon to which the R₃ group is attached is in the (S)configuration, and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted withone or more halo groups. In another embodiment, the Cyclo(hetero)alkenylCompound has an R₃ group, the R₃ group is attached to the carbon atom atthe 6-position of the tetrahydropiperidine ring, the carbon to which theR₃ group is attached is in the (S) configuration, and R₃ is —CH₃. Inanother embodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group,the R₃ group is attached to the carbon atom at the 6-position of thetetrahydropiperidine ring, the carbon to which the R₃ group is attachedis in the (S) configuration, and R₃ is —CF₃. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 6-position of the tetrahydropiperidine ring,the carbon to which the R₃ group is attached is in the (S)configuration, and R₃ is —CH₂CH₃.

In another embodiment, the Cyclo(hetero)alkenyl Compound has an R₃group, the R₃ group is attached to the carbon atom at the 5-position ofthe tetrahydropiperidine ring, and the carbon to which the R₃ group isattached is in the (S) configuration. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 5-position of the tetrahydropiperidine ring,the carbon to which the R₃ group is attached is in the (S)configuration, and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted withone or more halo groups. In another embodiment, the Cyclo(hetero)alkenylCompound has an R₃ group, the R₃ group is attached to the carbon atom atthe 5-position of the tetrahydropiperidine ring, the carbon to which theR₃ group is attached is in the (S) configuration, and R₃ is —CH₃. Inanother embodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group,the R₃ group is attached to the carbon atom at the 5-position of thetetrahydropiperidine ring, the carbon to which the R₃ group is attachedis in the (S) configuration, and R₃ is —CF₃. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 5-position of the tetrahydropiperidine ring,the carbon atom to which the R₃ group is attached is in the (S)configuration, and R₃ is —CH₂CH₃.

In another embodiment, the Cyclo(hetero)alkenyl Compound has an R₃group, the R₃ group is attached to the carbon atom at the 2-position ofthe cyclo(hetero)alkenyl ring and R₃ is —(C₁-C₄) alkyl unsubstituted orsubstituted with one or more halo groups. In another embodiment, theCyclo(hetero)alkenyl Compound has an R₃ group, the R₃ group is attachedto the carbon atom at the 2-position of the cyclo(hetero)alkenyl ringand R₃ is —CH₃. In another embodiment, the Cyclo(hetero)alkenyl Compoundhas an R₃ group, the R₃ group is attached to the carbon atom at the2-position of the cyclo(hetero)alkenyl ring and R₃ is —CF₃. In anotherembodiment, the Cyclo(hetero)alkenyl Compound has an R₃ group, the R₃group is attached to the carbon atom at the 2-position of thecyclo(hetero)alkenyl ring and R₃ is —CH₂CH₃.

4.1.2 Cyclo(Hetero)Alkenyl Compounds of Formula (IA)

The present invention encompasses Compounds of Formula (IA)

and pharmaceutically acceptable salts thereof, where V, Ar¹, Ar², R₃,and m are defined above for the Cyclo(hetero)alkenyl Compounds ofFormula (IA).

Illustrative Cyclo(hetero)alkenyl Compounds are listed below in Tables1-27.

For the chemical structure depicted, e.g., at the head of each of Tables1, 3, 5, 7, 9, 13-19, 21, 22, 24, 25 and 27, a is independently 0 or 1.When a=0, the group at the “a” position is —H. When a=1, the group atthe “a” position (R_(8a)) is other than —H, i.e., is R₈.

For the chemical structure depicted, e.g., at the head of each of Tables2, 4, 6, 8, 10, 20, 23 and 26, a is independently 0 or 1. When a=0, thegroup at the “a” position is —H. When a=1, the group at the “a” position((R₈)_(a)) is other than —H, i.e., is R₈.

For the chemical structure depicted, e.g., at the head of each of Tables2, 4, 6, 8, 10, 20, 23 and 26, b is independently 0 or 1. When b=0, thegroup at the “b” position is —H. When b=1, the group at the “b” position((R₈)_(b)) is other than —H, i.e., is R₈.

TABLE 1 (Ia)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a) A1 (a and b) —H —H A2 (a and b) —H -tert-butyl A3 (a and b) —H-iso-butyl A4 (a and b) —H -sec-butyl A5 (a and b) —H -iso-propyl A6 (aand b) —H -n-propyl A7 (a and b) —H -cyclohexyl A8 (a and b) —H-tert-butoxy A9 (a and b) —H -isopropoxy A10 (a and b) —H —CF₃ A11 (aand b) —H —CH₂CF₃ A12 (a and b) —H —OCF₃ A13 (a and b) —H —Cl A14 (a andb) —H —Br A15 (a and b) —H —I A16 (a and b) —H -n-butyl A17 (a and b) —H—CH₃ A18 (a and b) —H —SCF₃ A19 (a and b) —H —N(CH₂CH₃)₂ A20 (a and b)—H —OCF₂CHF₂ A21 (a and b) —H —C(OH)(CF₃)₂ A22 (a and b) —H-(1,1-dimethyl-pentyl) A23 (a and b) —H -(1,1-dimethyl-acetic acid)ethyl ester A24 (a and b) —H —N-piperidinyl A25 (a and b) —Cl —H A26 (aand b) —Cl -tert-butyl A27 (a and b) —Cl -iso-butyl A28 (a and b) —Cl-sec-butyl A29 (a and b) —Cl -iso-propyl A30 (a and b) —Cl -n-propyl A31(a and b) —Cl -cyclohexyl A32 (a and b) —Cl -tert-butoxy A33 (a and b)—Cl -isopropoxy A34 (a and b) —Cl —CF₃ A35 (a and b) —Cl —CH₂CF₃ A36 (aand b) —Cl —OCF₃ A37 (a and b) —Cl —Cl A38 (a and b) —Cl —Br A39 (a andb) —Cl —I A40 (a and b) —Cl -n-butyl A41 (a and b) —Cl —CH₃ A42 (a andb) —Cl —SCF₃ A43 (a and b) —Cl —N(CH₂CH₃)₂ A44 (a and b) —Cl —OCF₂CHF₂A45 (a and b) —Cl —C(OH)(CF₃)₂ A46 (a and b) —Cl -(1,1-dimethyl-pentyl)A47 (a and b) —Cl -(1,1-dimethyl-acetic acid) ethyl ester A48 (a and b)—Cl —N-piperidinyl A49 (a and b) —F —H A50 (a and b) —F -tert-butyl A51(a and b) —F -iso-butyl A52 (a and b) —F -sec-butyl A53 (a and b) —F-iso-propyl A54 (a and b) —F -n-propyl A55 (a and b) —F -cyclohexyl A56(a and b) —F -tert-butoxy A57 (a and b) —F -isopropoxy A58 (a and b) —F—CF₃ A59 (a and b) —F —CH₂CF₃ A60 (a and b) —F —OCF₃ A61 (a and b) —F—Cl A62 (a and b) —F —Br A63 (a and b) —F —I A64 (a and b) —F -n-butylA65 (a and b) —F —CH₃ A66 (a and b) —F —SCF₃ A67 (a and b) —F—N(CH₂CH₃)₂ A68 (a and b) —F —OCF₂CHF₂ A69 (a and b) —F —C(OH)(CF₃)₂ A70(a and b) —F -(1,1-dimethyl-pentyl) A71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester A72 (a and b) —F —N-piperidinylA73 (a and b) —CH₃ —H A74 (a and b) —CH₃ -tert-butyl A75 (a and b) —CH₃-iso-butyl A76 (a and b) —CH₃ -sec-butyl A77 (a and b) —CH₃ -iso-propylA78 (a and b) —CH₃ -n-propyl A79 (a and b) —CH₃ -cyclohexyl A80 (a andb) —CH₃ -tert-butoxy A81 (a and b) —CH₃ -isopropoxy A82 (a and b) —CH₃—CF₃ A83 (a and b) —CH₃ —CH₂CF₃ A84 (a and b) —CH₃ —OCF₃ A85 (a and b)—CH₃ —Cl A86 (a and b) —CH₃ —Br A87 (a and b) —CH₃ —I A88 (a and b) —CH₃-n-butyl A89 (a and b) —CH₃ —CH₃ A90 (a and b) —CH₃ —SCF₃ A91 (a and b)—CH₃ —N(CH₂CH₃)₂ A92 (a and b) —CH₃ —OCF₂CHF₂ A93 (a and b) —CH₃—C(OH)(CF₃)₂ A94 (a and b) —CH₃ -(1,1-dimethyl-pentyl) A95 (a and b)—CH₃ -(1,1-dimethyl-acetic acid) ethyl ester A96 (a and b) —CH₃—N-piperidinyl A97 (a and b) —CF₃ —H A98 (a and b) —CF₃ -tert-butyl A99(a and b) —CF₃ -iso-butyl A100 (a and b) —CF₃ -sec-butyl A101 (a and b)—CF₃ -iso-propyl A102 (a and b) —CF₃ -n-propyl A103 (a and b) —CF₃-cyclohexyl A104 (a and b) —CF₃ -tert-butoxy A105 (a and b) —CF₃-isopropoxy A106 (a and b) —CF₃ —CF₃ A107 (a and b) —CF₃ —CH₂CF₃ A108 (aand b) —CF₃ —OCF₃ A109 (a and b) —CF₃ —Cl A110 (a and b) —CF₃ —Br A111(a and b) —CF₃ —I A112 (a and b) —CF₃ -n-butyl A113 (a and b) —CF₃ —CH₃A114 (a and b) —CF₃ —SCF₃ A115 (a and b) —CF₃ —N(CH₂CH₃)₂ A116 (a and b)—CF₃ —OCF₂CHF₂ A117 (a and b) —CF₃ —C(OH)(CF₃)₂ A118 (a and b) —CF₃-(1,1-dimethyl-pentyl) A119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester A120 (a and b) —CF₃ —N-piperidinyl A121 (a and b) —CHF₂-tert-butyl A122 (a and b) —CHF₂ —H A123 (a and b) —CHF₂ -iso-butyl A124(a and b) —CHF₂ -sec-butyl A125 (a and b) —CHF₂ -iso-propyl A126 (a andb) —CHF₂ -n-propyl A127 (a and b) —CHF₂ -cyclohexyl A128 (a and b) —CHF₂-tert-butoxy A129 (a and b) —CHF₂ -isopropoxy A130 (a and b) —CHF₂ —CF₃A131 (a and b) —CHF₂ —CH₂CF₃ A132 (a and b) —CHF₂ —OCF₃ A133 (a and b)—CHF₂ —Cl A134 (a and b) —CHF₂ —Br A135 (a and b) —CHF₂ —I A136 (a andb) —CHF₂ -n-butyl A137 (a and b) —CHF₂ —CH₃ A138 (a and b) —CHF₂ —SCF₃A139 (a and b) —CHF₂ —N(CH₂CH₃)₂ A140 (a and b) —CHF₂ —OCF₂CHF₂ A141 (aand b) —CHF₂ —C(OH)(CF₃)₂ A142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)A143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester A144 (a andb) —CHF₂ —N-piperidinyl A145 (a and b) —OH —H A146 (a and b) —OH-tert-butyl A147 (a and b) —OH -iso-butyl A148 (a and b) —OH -sec-butylA149 (a and b) —OH -iso-propyl A150 (a and b) —OH -n-propyl A151 (a andb) —OH -cyclohexyl A152 (a and b) —OH -tert-butoxy A153 (a and b) —OH-isopropoxy A154 (a and b) —OH —CF₃ A155 (a and b) —OH —CH₂CF₃ A156 (aand b) —OH —OCF₃ A157 (a and b) —OH —Cl A158 (a and b) —OH —Br A159 (aand b) —OH —I A160 (a and b) —OH -n-butyl A161 (a and b) —OH —CH₃ A162(a and b) —OH —SCF₃ A163 (a and b) —OH —N(CH₂CH₃)₂ A164 (a and b) —OH—OCF₂CHF₂ A165 (a and b) —OH —C(OH)(CF₃)₂ A166 (a and b) —OH-(1,1-dimethyl-pentyl) A167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester A168 (a and b) —OH —N-piperidinyl A169 (a and b) —NO₂ —HA170 (a and b) —NO₂ -tert-butyl A171 (a and b) —NO₂ -iso-butyl A172 (aand b) —NO₂ -sec-butyl A173 (a and b) —NO₂ -iso-propyl A174 (a and b)—NO₂ -n-propyl A175 (a and b) —NO₂ -cyclohexyl A176 (a and b) —NO₂-tert-butoxy A177 (a and b) —NO₂ -isopropoxy A178 (a and b) —NO₂ —CF₃A179 (a and b) —NO₂ —CH₂CF₃ A180 (a and b) —NO₂ —OCF₃ A181 (a and b)—NO₂ —Cl A182 (a and b) —NO₂ —Br A183 (a and b) —NO₂ —I A184 (a and b)—NO₂ -n-butyl A185 (a and b) —NO₂ —CH₃ A186 (a and b) —NO₂ —SCF₃ A187 (aand b) —NO₂ —N(CH₂CH₃)₂ A188 (a and b) —NO₂ —OCF₂CHF₂ A189 (a and b)—NO₂ —C(OH)(CF₃)₂ A190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) A191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester A192 (a and b) —NO₂—N-piperidinyl A193 (a and b) —CN —H A194 (a and b) —CN -tert-butyl A195(a and b) —CN -iso-butyl A196 (a and b) —CN -sec-butyl A197 (a and b)—CN -iso-propyl A198 (a and b) —CN -n-propyl A199 (a and b) —CN-cyclohexyl A200 (a and b) —CN -tert-butoxy A201 (a and b) —CN-isopropoxy A202 (a and b) —CN —CF₃ A203 (a and b) —CN —CH₂CF₃ A204 (aand b) —CN —OCF₃ A205 (a and b) —CN —Cl A206 (a and b) —CN —Br A207 (aand b) —CN —I A208 (a and b) —CN -n-butyl A209 (a and b) —CN —CH₃ A210(a and b) —CN —SCF₃ A211 (a and b) —CN —N(CH₂CH₃)₂ A212 (a and b) —CN—OCF₂CHF₂ A213 (a and b) —CN —C(OH)(CF₃)₂ A214 (a and b) —CN-(1,1-dimethyl-pentyl) A215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester A216 (a and b) —CN —N-piperidinyl A217 (a and b) —Br —H A218(a and b) —Br -tert-butyl A219 (a and b) —Br -iso-butyl A220 (a and b)—Br -sec-butyl A221 (a and b) —Br -iso-propyl A222 (a and b) —Br-n-propyl A223 (a and b) —Br -cyclohexyl A224 (a and b) —Br -tert-butoxyA225 (a and b) —Br -isopropoxy A226 (a and b) —Br —CF₃ A227 (a and b)—Br —CH₂CF₃ A228 (a and b) —Br —OCF₃ A229 (a and b) —Br —Cl A230 (a andb) —Br —Br A231 (a and b) —Br —I A232 (a and b) —Br -n-butyl A233 (a andb) —Br —CH₃ A234 (a and b) —Br —SCF₃ A235 (a and b) —Br —N(CH₂CH₃)₂ A236(a and b) —Br —OCF₂CHF₂ A237 (a and b) —Br —C(OH)(CF₃)₂ A238 (a and b)—Br -(1,1-dimethyl-pentyl) A239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester A240 (a and b) —Br —N-piperidinyl A241 (a and b) —I-tert-butyl A242 (a and b) —I —H A243 (a and b) —I -iso-butyl A244 (aand b) —I -sec-butyl A245 (a and b) —I -iso-propyl A246 (a and b) —I-n-propyl A247 (a and b) —I -cyclohexyl A248 (a and b) —I -tert-butoxyA249 (a and b) —I -isopropoxy A250 (a and b) —I —CF₃ A251 (a and b) —I—CH₂CF₃ A252 (a and b) —I —OCF₃ A253 (a and b) —I —Cl A254 (a and b) —I—Br A255 (a and b) —I —I A256 (a and b) —I -n-butyl A257 (a and b) —I—CH₃ A258 (a and b) —I —SCF₃ A259 (a and b) —I —N(CH₂CH₃)₂ A260 (a andb) —I —OCF₂CHF₂ A261 (a and b) —I —C(OH)(CF₃)₂ A262 (a and b) —I-(1,1-dimethyl-pentyl) A263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester A264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 2 (Ib)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b) B01 (a and b) S —H —Cl —H B02 (a and b) S —H —Br —HB03 (a and b) S —H —F —H B04 (a and b) S —H —CH₃ —H B05 (a and b) S —H—CF₃ —H B06 (a and b) S —H —OCH₃ —H B07 (a and b) S —H —OCH₂CH₃ —H B08(a and b) S —H —OCF₃ —H B09 (a and b) S —H -tert-butyl —H B10 (a and b)S —H -iso-propyl —H B11 (a and b) S —H —CH₃ —CH₃ B12 (a and b) S —H —H—H B13 (a and b) S —H —H —Cl B14 (a and b) S —H —H —Br B15 (a and b) S—H —H —F B16 (a and b) S —H —H —CH₃ B17 (a and b) S —H —H —CF₃ B18 (aand b) S —H —H —OCH₃ B19 (a and b) S —H —H —OCH₂CH₃ B20 (a and b) S —H—H —OCF₃ B21 (a and b) S —H —H -tert-butyl B22 (a and b) S —H —H-iso-propyl B23 (a and b) S —Cl —Cl —H B24 (a and b) S —Cl —Br —H B25 (aand b) S —Cl —F —H B26 (a and b) S —Cl —CH₃ —H B27 (a and b) S —Cl —CF₃—H B28 (a and b) S —Cl —OCH₃ —H B29 (a and b) S —Cl —OCH₂CH₃ —H B30 (aand b) S —Cl —OCF₃ —H B31 (a and b) S —Cl -tert-butyl —H B32 (a and b) S—Cl -iso-propyl —H B33 (a and b) S —Cl —CH₃ —CH₃ B34 (a and b) S —Cl —H—H B35 (a and b) S —Cl —H —Cl B36 (a and b) S —Cl —H —Br B37 (a and b) S—Cl —H —F B38 (a and b) S —Cl —H —CH₃ B39 (a and b) S —Cl —H —CF₃ B40 (aand b) S —Cl —H —OCH₃ B41 (a and b) S —Cl —H —OCH₂CH₃ B42 (a and b) S—Cl —H —OCF₃ B43 (a and b) S —Cl —H -tert-butyl B44 (a and b) S —Cl —H-iso-propyl B45 (a and b) S —Cl —H —OCF₃ B46 (a and b) S —Cl —H-tert-butyl B47 (a and b) S —Cl —H -iso-propyl B48 (a and b) S —CH₃ —Cl—H B49 (a and b) S —CH₃ —Br —H B50 (a and b) S —CH₃ —F —H B51 (a and b)S —CH₃ —CH₃ —H B52 (a and b) S —CH₃ —CF₃ —H B53 (a and b) S —CH₃ —OCH₃—H B54 (a and b) S —CH₃ —OCH₂CH₃ —H B55 (a and b) S —CH₃ —OCF₃ —H B56 (aand b) S —CH₃ -tert-butyl —H B57 (a and b) S —CH₃ -iso-propyl —H B58 (aand b) S —CH₃ —CH₃ —CH₃ B59 (a and b) S —CH₃ —H —H B60 (a and b) S —CH₃—H —Cl B61 (a and b) S —CH₃ —H —Br B62 (a and b) S —CH₃ —H —F B63 (a andb) S —CH₃ —H —CH₃ B64 (a and b) S —CH₃ —H —CF₃ B65 (a and b) S —CH₃ —H—OCH₃ B66 (a and b) S —CH₃ —H —OCH₂CH₃ B67 (a and b) S —CH₃ —H —OCF₃ B68(a and b) S —CH₃ —H -tert-butyl B69 (a and b) S —CH₃ —H -iso-propyl B70(a and b) S —CF₃ —Cl —H B71 (a and b) S —CF₃ —Br —H B72 (a and b) S —CF₃—F —H B73 (a and b) S —CF₃ —CH₃ —H B74 (a and b) S —CF₃ —CF₃ —H B75 (aand b) S —CF₃ —OCH₃ —H B76 (a and b) S —CF₃ —OCH₂CH₃ —H B77 (a and b) S—CF₃ —OCF₃ —H B78 (a and b) S —CF₃ -tert-butyl —H B79 (a and b) S —CF₃-iso-propyl —H B80 (a and b) S —CF₃ —CH₃ —CH₃ B81 (a and b) S —CF₃ —H —HB82 (a and b) S —CF₃ —H —Cl B83 (a and b) S —CF₃ —H —Br B84 (a and b) S—CF₃ —H —F B85 (a and b) S —CF₃ —H —CH₃ B86 (a and b) S —CF₃ —H —CF₃ B87(a and b) S —CF₃ —H —OCH₃ B88 (a and b) S —CF₃ —H —OCH₂CH₃ B89 (a and b)S —CF₃ —H —OCF₃ B90 (a and b) S —CF₃ —H -tert-butyl B91 (a and b) S —CF₃—H -iso-propyl B92 (a and b) S —CHF₂ —Cl —H B93 (a and b) S —CHF₂ —Br —HB94 (a and b) S —CHF₂ —F —H B95 (a and b) S —CHF₂ —CH₃ —H B96 (a and b)S —CHF₂ —CF₃ —H B97 (a and b) S —CHF₂ —OCH₃ —H B98 (a and b) S —CHF₂—OCH₂CH₃ —H B99 (a and b) S —CHF₂ —OCF₃ —H B100 (a and b) S —CHF₂-tert-butyl —H B101 (a and b) S —CHF₂ -iso-propyl —H B102 (a and b) S—CHF₂ —CH₃ —CH₃ B103 (a and b) S —CHF₂ —H —H B104 (a and b) S —CHF₂ —H—Cl B105 (a and b) S —CHF₂ —H —Br B106 (a and b) S —CHF₂ —H —F B107 (aand b) S —CHF₂ —H —CH₃ B108 (a and b) S —CHF₂ —H —CF₃ B109 (a and b) S—CHF₂ —H —OCH₃ B110 (a and b) S —CHF₂ —H —OCH₂CH₃ B111 (a and b) S —CHF₂—H —OCF₃ B112 (a and b) S —CHF₂ —H -tert-butyl B113 (a and b) S —CHF₂ —H-iso-propyl B114 (a and b) S —OH —Cl —H B115 (a and b) S —OH —Br —H B116(a and b) S —OH —F —H B117 (a and b) S —OH —CH₃ —H B118 (a and b) S —OH—CF₃ —H B119 (a and b) S —OH —OCH₃ —H B120 (a and b) S —OH —OCH₂CH₃ —HB121 (a and b) S —OH —OCF₃ —H B122 (a and b) S —OH -tert-butyl —H B123(a and b) S —OH -iso-propyl —H B124 (a and b) S —OH —CH₃ —CH₃ B125 (aand b) S —OH —H —H B126 (a and b) S —OH —H —Cl B127 (a and b) S —OH —H—Br B128 (a and b) S —OH —H —F B129 (a and b) S —OH —H —CH₃ B130 (a andb) S —OH —H —CF₃ B131 (a and b) S —OH —H —OCH₃ B132 (a and b) S —OH —H—OCH₂CH₃ B133 (a and b) S —OH —H —OCF₃ B134 (a and b) S —OH —H-tert-butyl B135 (a and b) S —OH —H -iso-propyl B136 (a and b) S —NO₂—Cl —H B137 (a and b) S —NO₂ —Br —H B138 (a and b) S —NO₂ —F —H B139 (aand b) S —NO₂ —CH₃ —H B140 (a and b) S —NO₂ —CF₃ —H B141 (a and b) S—NO₂ —OCH₃ —H B142 (a and b) S —NO₂ —OCH₂CH₃ —H B143 (a and b) S —NO₂—OCF₃ —H B144 (a and b) S —NO₂ -tert-butyl —H B145 (a and b) S —NO₂-iso-propyl —H B146 (a and b) S —NO₂ —CH₃ —CH₃ B147 (a and b) S —NO₂ —H—H B148 (a and b) S —NO₂ —H —Cl B149 (a and b) S —NO₂ —H —Br B150 (a andb) S —NO₂ —H —F B151 (a and b) S —NO₂ —H —CH₃ B152 (a and b) S —NO₂ —H—CF₃ B153 (a and b) S —NO₂ —H —OCH₃ B154 (a and b) S —NO₂ —H —OCH₂CH₃B155 (a and b) S —NO₂ —H —OCF₃ B156 (a and b) S —NO₂ —H -tert-butyl B157(a and b) S —NO₂ —H -iso-propyl B158 (a and b) S —CN —Br —H B159 (a andb) S —CN —Cl —H B160 (a and b) S —CN —F —H B161 (a and b) S —CN —CH₃ —HB162 (a and b) S —CN —CF₃ —H B163 (a and b) S —CN —OCH₃ —H B164 (a andb) S —CN —OCH₂CH₃ —H B165 (a and b) S —CN —OCF₃ —H B166 (a and b) S —CN-tert-butyl —H B167 (a and b) S —CN -iso-propyl —H B168 (a and b) S —CN—CH₃ —CH₃ B169 (a and b) S —CN —H —H B170 (a and b) S —CN —H —Cl B171 (aand b) S —CN —H —Br B172 (a and b) S —CN —H —F B173 (a and b) S —CN —H—CH₃ B174 (a and b) S —CN —H —CF₃ B175 (a and b) S —CN —H —OCH₃ B176 (aand b) S —CN —H —OCH₂CH₃ B177 (a and b) S —CN —H —OCF₃ B178 (a and b) S—CN —H -tert-butyl B179 (a and b) S —CN —H -iso-propyl B180 (a and b) S—Br —Br —H B181 (a and b) S —Br —Cl —H B182 (a and b) S —Br —F —H B183(a and b) S —Br —CH₃ —H B184 (a and b) S —Br —CF₃ —H B185 (a and b) S—Br —OCH₃ —H B186 (a and b) S —Br —OCH₂CH₃ —H B187 (a and b) S —Br —OCF₃—H B188 (a and b) S —Br -tert-butyl —H B189 (a and b) S —Br -iso-propyl—H B190 (a and b) S —Br —CH₃ —CH₃ B191 (a and b) S —Br —H —H B192 (a andb) S —Br —H —Cl B193 (a and b) S —Br —H —Br B194 (a and b) S —Br —H —FB195 (a and b) S —Br —H —CH₃ B196 (a and b) S —Br —H —CF₃ B197 (a and b)S —Br —H —OCH₃ B198 (a and b) S —Br —H —OCH₂CH₃ B199 (a and b) S —Br —H—OCF₃ B200 (a and b) S —Br —H -tert-butyl B201 (a and b) S —Br —H-iso-propyl B202 (a and b) S —I —Cl —H B203 (a and b) S —I —Br —H B204(a and b) S —I —F —H B205 (a and b) S —I —CH₃ —H B206 (a and b) S —I—CF₃ —H B207 (a and b) S —I —OCH₃ —H B208 (a and b) S —I —OCH₂CH₃ —HB209 (a and b) S —I —OCF₃ —H B210 (a and b) S —I -tert-butyl —H B211 (aand b) S —I -iso-propyl —H B212 (a and b) S —I —CH₃ —CH₃ B213 (a and b)S —I —H —H B214 (a and b) S —I —H —Cl B215 (a and b) S —I —H —Br B216 (aand b) S —I —H —F B217 (a and b) S —I —H —CH₃ B218 (a and b) S —I —H—CF₃ B219 (a and b) S —I —H —OCH₃ B220 (a and b) S —I —H —OCH₂CH₃ B221(a and b) S —I —H —OCF₃ B222 (a and b) S —I —H -tert-butyl B223 (a andb) S —I —H -iso-propyl B224 (a and b) O —H —Cl —H B225 (a and b) O —H—Br —H B226 (a and b) O —H —F —H B227 (a and b) O —H —CH₃ —H B228 (a andb) O —H —CF₃ —H B229 (a and b) O —H —OCH₃ —H B230 (a and b) O —H—OCH₂CH₃ —H B231 (a and b) O —H —OCF₃ —H B232 (a and b) O —H -tert-butyl—H B233 (a and b) O —H -iso-propyl —H B234 (a and b) O —H —CH₃ —CH₃ B235(a and b) O —H —H —H B236 (a and b) O —H —H —Cl B237 (a and b) O —H —H—Br B238 (a and b) O —H —H —F B239 (a and b) O —H —H —CH₃ B240 (a and b)O —H —H —CF₃ B241 (a and b) O —H —H —OCH₃ B242 (a and b) O —H —H—OCH₂CH₃ B243 (a and b) O —H —H —OCF₃ B244 (a and b) O —H —H -tert-butylB245 (a and b) O —H —H -iso-propyl B246 (a and b) O —Cl —Cl —H B247 (aand b) O —Cl —Br —H B248 (a and b) O —Cl —F —H B249 (a and b) O —Cl —CH₃—H B250 (a and b) O —Cl —CF₃ —H B251 (a and b) O —Cl —OCH₃ —H B252 (aand b) O —Cl —OCH₂CH₃ —H B253 (a and b) O —Cl —OCF₃ —H B254 (a and b) O—Cl -tert-butyl —H B255 (a and b) O —Cl -iso-propyl —H B256 (a and b) O—Cl —CH₃ —CH₃ B257 (a and b) O —Cl —H —H B258 (a and b) O —Cl —H —CH₃B259 (a and b) O —Cl —H —Cl B260 (a and b) O —Cl —H —Br B261 (a and b) O—Cl —H —F B262 (a and b) O —Cl —H —CF₃ B263 (a and b) O —Cl —H —OCH₃B264 (a and b) O —Cl —H —OCH₂CH₃ B265 (a and b) O —Cl —H —OCF₃ B266 (aand b) O —Cl —H -tert-butyl B267 (a and b) O —Cl —H -iso-propyl B268 (aand b) O —Cl —H —OCF₃ B269 (a and b) O —Cl —H -tert-butyl B270 (a and b)O —Cl —H -iso-propyl B271 (a and b) O —CH₃ —Cl —H B272 (a and b) O —CH₃—Br —H B273 (a and b) O —CH₃ —F —H B274 (a and b) O —CH₃ —CH₃ —H B275 (aand b) O —CH₃ —CF₃ —H B276 (a and b) O —CH₃ —OCH₃ —H B277 (a and b) O—CH₃ —OCH₂CH₃ —H B278 (a and b) O —CH₃ —OCF₃ —H B279 (a and b) O —CH₃-tert-butyl —H B280 (a and b) O —CH₃ -iso-propyl —H B281 (a and b) O—CH₃ —CH₃ —CH₃ B282 (a and b) O —CH₃ —H —H B283 (a and b) O —CH₃ —H —ClB284 (a and b) O —CH₃ —H —Br B285 (a and b) O —CH₃ —H —F B286 (a and b)O —CH₃ —H —CH₃ B287 (a and b) O —CH₃ —H —CF₃ B288 (a and b) O —CH₃ —H—OCH₃ B289 (a and b) O —CH₃ —H —OCH₂CH₃ B290 (a and b) O —CH₃ —H —OCF₃B291 (a and b) O —CH₃ —H -tert-butyl B292 (a and b) O —CH₃ —H-iso-propyl B293 (a and b) O —CF₃ —Cl —H B294 (a and b) O —CF₃ —Br —HB295 (a and b) O —CF₃ —F —H B296 (a and b) O —CF₃ —CH₃ —H B297 (a and b)O —CF₃ —CF₃ —H B298 (a and b) O —CF₃ —OCH₃ —H B299 (a and b) O —CF₃—OCH₂CH₃ —H B300 (a and b) O —CF₃ —OCF₃ —H B301 (a and b) O —CF₃-tert-butyl —H B302 (a and b) O —CF₃ -iso-propyl —H B303 (a and b) O—CF₃ —CH₃ —CH₃ B304 (a and b) O —CF₃ —H —H B305 (a and b) O —CF₃ —H —ClB306 (a and b) O —CF₃ —H —Br B307 (a and b) O —CF₃ —H —F B308 (a and b)O —CF₃ —H —CH₃ B309 (a and b) O —CF₃ —H —CF₃ B310 (a and b) O —CF₃ —H—OCH₃ B311 (a and b) O —CF₃ —H —OCH₂CH₃ B312 (a and b) O —CF₃ —H —OCF₃B313 (a and b) O —CF₃ —H -tert-butyl B314 (a and b) O —CF₃ —H-iso-propyl B315 (a and b) O —CHF₂ —Cl —H B316 (a and b) O —CHF₂ —Br —HB317 (a and b) O —CHF₂ —F —H B318 (a and b) O —CHF₂ —CH₃ —H B319 (a andb) O —CHF₂ —CF₃ —H B320 (a and b) O —CHF₂ —OCH₃ —H B321 (a and b) O—CHF₂ —OCH₂CH₃ —H B322 (a and b) O —CHF₂ —OCF₃ —H B323 (a and b) O —CHF₂-tert-butyl —H B324 (a and b) O —CHF₂ -iso-propyl —H B325 (a and b) O—CHF₂ —CH₃ —CH₃ B326 (a and b) O —CHF₂ —H —H B327 (a and b) O —CHF₂ —H—Cl B328 (a and b) O —CHF₂ —H —Br B329 (a and b) O —CHF₂ —H —F B330 (aand b) O —CHF₂ —H —CH₃ B331 (a and b) O —CHF₂ —H —CF₃ B332 (a and b) O—CHF₂ —H —OCH₃ B333 (a and b) O —CHF₂ —H —OCH₂CH₃ B334 (a and b) O —CHF₂—H —OCF₃ B335 (a and b) O —CHF₂ —H -tert-butyl B336 (a and b) O —CHF₂ —H-iso-propyl B337 (a and b) O —OH —Cl —H B338 (a and b) O —OH —Br —H B339(a and b) O —OH —F —H B340 (a and b) O —OH —CH₃ —H B341 (a and b) O —OH—CF₃ —H B342 (a and b) O —OH —OCH₃ —H B343 (a and b) O —OH —OCH₂CH₃ —HB344 (a and b) O —OH —OCF₃ —H B345 (a and b) O —OH -tert-butyl —H B346(a and b) O —OH -iso-propyl —H B347 (a and b) O —OH —CH₃ —CH₃ B348 (aand b) O —OH —H —H B349 (a and b) O —OH —H —Cl B350 (a and b) O —OH —H—Br B351 (a and b) O —OH —H —F B352 (a and b) O —OH —H —CH₃ B353 (a andb) O —OH —H —CF₃ B354 (a and b) O —OH —H —OCH₃ B355 (a and b) O —OH —H—OCH₂CH₃ B356 (a and b) O —OH —H —OCF₃ B357 (a and b) O —OH —H-tert-butyl B358 (a and b) O —OH —H -iso-propyl B359 (a and b) O —NO₂—Cl —H B360 (a and b) O —NO₂ —Br —H B361 (a and b) O —NO₂ —F —H B362 (aand b) O —NO₂ —CH₃ —H B363 (a and b) O —NO₂ —CF₃ —H B364 (a and b) O—NO₂ —OCH₃ —H B365 (a and b) O —NO₂ —OCH₂CH₃ —H B366 (a and b) O —NO₂—OCF₃ —H B367 (a and b) O —NO_(2.) -tert-butyl —H B368 (a and b) O —NO₂-iso-propyl —H B369 (a and b) O —NO₂ —CH₃ —CH₃ B370 (a and b) O —NO₂ —H—H B371 (a and b) O —NO₂ —H —Cl B372 (a and b) O —NO₂ —H —Br B373 (a andb) O —NO₂ —H —F B374 (a and b) O —NO₂ —H —CH₃ B375 (a and b) O —NO₂ —H—CF₃ B376 (a and b) O —NO₂ —H —OCH₃ B377 (a and b) O —NO₂ —H —OCH₂CH₃B378 (a and b) O —NO₂ —H —OCF₃ B379 (a and b) O —NO₂ —H -tert-butyl B380(a and b) O —NO₂ —H -iso-propyl B381 (a and b) O —CN —Br —H B382 (a andb) O —CN —Cl —H B383 (a and b) O —CN —F —H B384 (a and b) O —CN —CH₃ —HB385 (a and b) O —CN —CF₃ —H B386 (a and b) O —CN —OCH₃ —H B387 (a andb) O —CN —OCH₂CH₃ —H B388 (a and b) O —CN —OCF₃ —H B389 (a and b) O —CN-tert-butyl —H B390 (a and b) O —CN -iso-propyl —H B391 (a and b) O —CN—CH₃ —CH₃ B392 (a and b) O —CN —H —H B393 (a and b) O —CN —H —Cl B394 (aand b) O —CN —H —Br B395 (a and b) O —CN —H —F B396 (a and b) O —CN —H—CH₃ B397 (a and b) O —CN —H —CF₃ B398 (a and b) O —CN —H —OCH₃ B399 (aand b) O —CN —H —OCH₂CH₃ B400 (a and b) O —CN —H —OCF₃ B401 (a and b) O—CN —H -tert-butyl B402 (a and b) O —CN —H -iso-propyl B403 (a and b) O—Br —Br —H B404 (a and b) O —Br —Cl —H B405 (a and b) O —Br —F —H B406(a and b) O —Br —CH₃ —H B407 (a and b) O —Br —CF₃ —H B408 (a and b) O—Br —OCH₃ —H B409 (a and b) O —Br —OCH₂CH₃ —H B410 (a and b) O —Br —OCF₃—H B411 (a and b) O —Br -tert-butyl —H B412 (a and b) O —Br -iso-propyl—H B413 (a and b) O —Br —CH₃ —CH₃ B414 (a and b) O —Br —H —H B415 (a andb) O —Br —H —Cl B416 (a and b) O —Br —H —Br B417 (a and b) O —Br —H —FB418 (a and b) O —Br —H —CH₃ B419 (a and b) O —Br —H —CF₃ B420 (a and b)O —Br —H —OCH₃ B421 (a and b) O —Br —H —OCH₂CH₃ B422 (a and b) O —Br —H—OCF₃ B423 (a and b) O —Br —H -tert-butyl B424 (a and b) O —Br —H-iso-propyl B425 (a and b) O —I —Cl —H B426 (a and b) O —I —Br —H B427(a and b) O —I —F —H B428 (a and b) O —I —CH₃ —H B429 (a and b) O —I—CF₃ —H B430 (a and b) O —I —OCH₃ —H B431 (a and b) O —I —OCH₂CH₃ —HB432 (a and b) O —I —OCF₃ —H B433 (a and b) O —I -tert-butyl —H B434 (aand b) O —I -iso-propyl —H B435 (a and b) O —I —CH₃ —CH₃ B436 (a and b)O —I —H —H B437 (a and b) O —I —H —Cl B438 (a and b) O —I —H —Br B439 (aand b) O —I —H —F B440 (a and b) O —I —H —CH₃ B441 (a and b) O —I —H—OCF₃ B442 (a and b) O —I —H —OCH₃ B443 (a and b) O —I —H —OCH₂CH₃ B444(a and b) O —I —H —OCF₃ B445 (a and b) O —I —H -tert-butyl B446 (a andb) O —I —H -iso-propyl B447 (a and b) NH —H —Cl —H B448 (a and b) NH —H—Br —H B449 (a and b) NH —H —F —H B450 (a and b) NH —H —CH₃ —H B451 (aand b) NH —H —CF₃ —H B452 (a and b) NH —H —OCH₃ —H B453 (a and b) NH —H—OCH₂CH₃ —H B454 (a and b) NH —H —OCF₃ —H B455 (a and b) NH —H-tert-butyl —H B456 (a and b) NH —H -iso-propyl —H B457 (a and b) NH —H—CH₃ —CH₃ B458 (a and b) NH —H —H —H B459 (a and b) NH —H —H —Cl B460 (aand b) NH —H —H —Br B461 (a and b) NH —H —H —F B462 (a and b) NH —H —H—CH₃ B463 (a and b) NH —H —H —CF₃ B464 (a and b) NH —H —H —OCH₃ B465 (aand b) NH —H —H —OCH₂CH₃ B466 (a and b) NH —H —H —OCF₃ B467 (a and b) NH—H —H -tert-butyl B468 (a and b) NH —H —H -iso-propyl B469 (a and b) NH—Cl —Cl —H B470 (a and b) NH —Cl —Br —H B471 (a and b) NH —Cl —F —H B472(a and b) NH —Cl —CH₃ —H B473 (a and b) NH —Cl —CF₃ —H B474 (a and b) NH—Cl —OCH₃ —H B475 (a and b) NH —Cl —OCH₂CH₃ —H B476 (a and b) NH —Cl—OCF₃ —H B477 (a and b) NH —Cl -tert-butyl —H B478 (a and b) NH —Cl-iso-propyl —H B479 (a and b) NH —Cl —CH₃ —CH₃ B480 (a and b) NH —Cl —H—H B481 (a and b) NH —Cl —H —CH₃ B482 (a and b) NH —Cl —H —Cl B483 (aand b) NH —Cl —H —Br B484 (a and b) NH —Cl —H —F B485 (a and b) NH —Cl—H —CF₃ B486 (a and b) NH —Cl —H —OCH₃ B487 (a and b) NH —Cl —H —OCH₂CH₃B488 (a and b) NH —Cl —H —OCF₃ B489 (a and b) NH —Cl —H -tert-butyl B490(a and b) NH —Cl —H -iso-propyl B491 (a and b) NH —Cl —H —OCF₃ B492 (aand b) NH —Cl —H -tert-butyl B493 (a and b) NH —Cl —H -iso-propyl B494(a and b) NH —CH₃ —Cl —H B495 (a and b) NH —CH₃ —Br —H B496 (a and b) NH—CH₃ —F —H B497 (a and b) NH —CH₃ —CH₃ —H B498 (a and b) NH —CH₃ —CF₃ —HB499 (a and b) NH —CH₃ —OCH₃ —H B500 (a and b) NH —CH₃ —OCH₂CH₃ —H B501(a and b) NH —CH₃ —OCF₃ —H B502 (a and b) NH —CH₃ -tert-butyl —H B503 (aand b) NH —CH₃ -iso-propyl —H B504 (a and b) NH —CH₃ —CH₃ —CH₃ B505 (aand b) NH —CH₃ —H —H B506 (a and b) NH —CH₃ —H —Cl B507 (a and b) NH—CH₃ —H —Br B508 (a and b) NH —CH₃ —H —F B509 (a and b) NH —CH₃ —H —CH₃B510 (a and b) NH —CH₃ —H —CF₃ B511 (a and b) NH —CH₃ —H —OCH₃ B512 (aand b) NH —CH₃ —H —OCH₂CH₃ B513 (a and b) NH —CH₃ —H —OCF₃ B514 (a andb) NH —CH₃ —H -tert-butyl B515 (a and b) NH —CH₃ —H -iso-propyl B516 (aand b) NH —CF₃ —Cl —H B517 (a and b) NH —CF₃ —Br —H B518 (a and b) NH—CF₃ —F —H B519 (a and b) NH —CF₃ —CH₃ —H B520 (a and b) NH —CF₃ —CF₃ —HB521 (a and b) NH —CF₃ —OCH₃ —H B522 (a and b) NH —CF₃ —OCH₂CH₃ —H B523(a and b) NH —CF₃ —OCF₃ —H B524 (a and b) NH —CF₃ -tert-butyl —H B525 (aand b) NH —CF₃ -iso-propyl —H B526 (a and b) NH —CF₃ —CH₃ —CH₃ B527 (aand b) NH —CF₃ —H —H B528 (a and b) NH —CF₃ —H —Cl B529 (a and b) NH—CF₃ —H —Br B530 (a and b) NH —CF₃ —H —F B531 (a and b) NH —CF₃ —H —CH₃B532 (a and b) NH —CF₃ —H —CF₃ B533 (a and b) NH —CF₃ —H —OCH₃ B534 (aand b) NH —CF₃ —H —OCH₂CH₃ B535 (a and b) NH —CF₃ —H —OCF₃ B536 (a andb) NH —CF₃ —H -tert-butyl B537 (a and b) NH —CF₃ —H -iso-propyl B538 (aand b) NH —CHF₂ —Cl —H B539 (a and b) NH —CHF₂ —Br —H B540 (a and b) NH—CHF₂ —F —H B541 (a and b) NH —CHF₂ —CH₃ —H B542 (a and b) NH —CHF₂ —CF₃—H B543 (a and b) NH —CHF₂ —OCH₃ —H B544 (a and b) NH —CHF₂ —OCH₂CH₃ —HB545 (a and b) NH —CHF₂ —OCF₃ —H B546 (a and b) NH —CHF₂ -tert-butyl —HB547 (a and b) NH —CHF₂ -iso-propyl —H B548 (a and b) NH —CHF₂ —CH₃ —CH₃B549 (a and b) NH —CHF₂ —H —H B550 (a and b) NH —CHF₂ —H —Cl B551 (a andb) NH —CHF₂ —H —Br B552 (a and b) NH —CHF₂ —H —F B553 (a and b) NH —CHF₂—H —CH₃ B554 (a and b) NH —CHF₂ —H —CF₃ B555 (a and b) NH —CHF₂ —H —OCH₃B556 (a and b) NH —CHF₂ —H —OCH₂CH₃ B557 (a and b) NH —CHF₂ —H —OCF₃B558 (a and b) NH —CHF₂ —H -tert-butyl B559 (a and b) NH —CHF₂ —H-iso-propyl B560 (a and b) NH —OH —C1 —H B561 (a and b) NH —OH —Br —HB562 (a and b) NH —OH —F —H B563 (a and b) NH —OH —CH₃ —H B564 (a and b)NH —OH —CF₃ —H B565 (a and b) NH —OH —OCH₃ —H B566 (a and b) NH —OH—OCH₂CH₃ —H B567 (a and b) NH —OH —OCF₃ —H B568 (a and b) NH —OH-tert-butyl —H B569 (a and b) NH —OH -iso-propyl —H B570 (a and b) NH—OH —CH₃ —CH₃ B571 (a and b) NH —OH —H —H B572 (a and b) NH —OH —H —ClB573 (a and b) NH —OH —H —Br B574 (a and b) NH —OH —H —F B575 (a and b)NH —OH —H —CH₃ B576 (a and b) NH —OH —H —CF₃ B577 (a and b) NH —OH —H—OCH₃ B578 (a and b) NH —OH —H —OCH₂CH₃ B579 (a and b) NH —OH —H —OCF₃B580 (a and b) NH —OH —H -tert-butyl B581 (a and b) NH —OH —H-iso-propyl B582 (a and b) NH —NO₂ —C1 —H B583 (a and b) NH —NO₂ —Br —HB584 (a and b) NH —NO₂ —F —H B585 (a and b) NH —NO₂ —CH₃ —H B586 (a andb) NH —NO₂ —CF₃ —H B587 (a and b) NH —NO₂ —OCH₃ —H B588 (a and b) NH—NO₂ —OCH₂CH₃ —H B589 (a and b) NH —NO₂ —OCF₃ —H B590 (a and b) NH —NO₂-tert-butyl —H BS91 (a and b) NH —NO₂ -iso-propyl —H B592 (a and b) NH—NO₂ —CH₃ —CH₃ B593 (a and b) NH —NO₂ —H —H B594 (a and b) NH —NO₂ —H—Cl B595 (a and b) NH —NO₂ —H —Br B596 (a and b) NH —NO₂ —H —F B597 (aand b) NH —NO₂ —H —CH₃ B598 (a and b) NH —NO₂ —H —CF₃ B599 (a and b) NH—NO₂ —H —OCH₃ B600 (a and b) NH —NO₂ —H —OCH₂CH₃ B601 (a and b) NH —NO₂—H —OCF₃ B602 (a and b) NH —NO₂ —H -tert-butyl B603 (a and b) NH —NO₂ —H-iso-propyl B604 (a and b) NH —CN —Br —H B605 (a and b) NH —CN —Cl —HB606 (a and b) NH —CN —F —H B607 (a and b) NH —CN —CH₃ —H B608 (a and b)NH —CN —CF₃ —H B609 (a and b) NH —CN —OCH₃ —H B610 (a and b) NH —CN—OCH₂CH₃ —H B611 (a and b) NH —CN —OCF₃ —H B612 (a and b) NH —CN-tert-butyl —H B613 (a and b) NH —CN -iso-propyl —H B614 (a and b) NH—CN —CH₃ —CH₃ B615 (a and b) NH —CN —H —H B616 (a and b) NH —CN —H —ClB617 (a and b) NH —CN —H —Br B618 (a and b) NH —CN —H —F B619 (a and b)NH —CN —H —CH₃ B620 (a and b) NH —CN —H —CF₃ B621 (a and b) NH —CN —H—OCH₃ B622 (a and b) NH —CN —H —OCH₂CH₃ B623 (a and b) NH —CN —H —OCF₃B624 (a and b) NH —CN —H -tert-butyl B625 (a and b) NH —CN —H-iso-propyl B626 (a and b) NH —Br —Br —H B627 (a and b) NH —Br —Cl —HB628 (a and b) NH —Br —F —H B629 (a and b) NH —Br —CH₃ —H B630 (a and b)NH —Br —CF₃ —H B631 (a and b) NH —Br —OCH₃ —H B632 (a and b) NH —Br—OCH₂CH₃ —H B633 (a and b) NH —Br —OCF₃ —H B634 (a and b) NH —Br-tert-butyl —H B635 (a and b) NH —Br -iso-propyl —H B636 (a and b) NH—Br —CH₃ —CH₃ B637 (a and b) NH —Br —H —H B638 (a and b) NH —Br —H —ClB639 (a and b) NH —Br —H —Br B640 (a and b) NH —Br —H —F B641 (a and b)NH —Br —H —CH₃ B642 (a and b) NH —Br —H —CF₃ B643 (a and b) NH —Br —H—OCH₃ B644 (a and b) NH —Br —H —OCH₂CH₃ B645 (a and b) NH —Br —H —OCF₃B646 (a and b) NH —Br —H -tert-butyl B647 (a and b) NH —Br —H-iso-propyl B648 (a and b) NH —I —Cl —H B649 (a and b) NH —I —Br —H B650(a and b) NH —I —F —H B651 (a and b) NH —I —CH₃ —H B652 (a and b) NH —I—CF₃ —H B653 (a and b) NH —I —OCH₃ —H B654 (a and b) NH —I —OCH₂CH₃ —HB655 (a and b) NH —I —OCF₃ —H B656 (a and b) NH —I -tert-butyl —H B657(a and b) NH —I -iso-propyl —H B658 (a and b) NH —I —CH₃ —CH₃ B659 (aand b) NH —I —H —H B660 (a and b) NH —I —H —Cl B661 (a and b) NH —I —H—Br B662 (a and b) NH —I —H —F B663 (a and b) NH —I —H —CH₃ B664 (a andb) NH —I —H —CF₃ B665 (a and b) NH —I —H —OCH₃ B666 (a and b) NH —I —H—OCH₂CH₃ B667 (a and b) NH —I —H —OCF₃ B668 (a and b) NH —I —H-tert-butyl B669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 3 (Ic)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a) C01 (a and b) —H —H C02 (a and b) —H -tert-butyl C03 (a and b) —H-iso-butyl C04 (a and b) —H -sec-butyl C05 (a and b) —H -iso-propyl C06(a and b) —H -n-propyl C07 (a and b) —H -cyclohexyl C08 (a and b) —H-tert-butoxy C09 (a and b) —H -isopropoxy C10 (a and b) —H —CF₃ C11 (aand b) —H —CH₂CF₃ C12 (a and b) —H —OCF₃ C13 (a and b) —H —Cl C14 (a andb) —H —Br C15 (a and b) —H —I C16 (a and b) —H -n-butyl C17 (a and b) —H—CH₃ C18 (a and b) —H —SCF₃ C19 (a and b) —H —N(CH₂CH₃)₂ C20 (a and b)—H —OCF₂CHF₂ C21 (a and b) —H —C(OH)(CF₃)₂ C22 (a and b) —H-(1,1-dimethyl-pentyl) C23 (a and b) —H -(1,1-dimethyl-acetic acid)ethyl ester C24 (a and b) —H —N-piperidinyl C25 (a and b) —Cl —H C26 (aand b) —Cl -tert-butyl C27 (a and b) —Cl -iso-butyl C28 (a and b) —Cl-sec-butyl C29 (a and b) —Cl -iso-propyl C30 (a and b) —Cl -n-propyl C31(a and b) —Cl -cyclohexyl C32 (a and b) —Cl -tert-butoxy C33 (a and b)—Cl -isopropoxy C34 (a and b) —Cl —CF₃ C35 (a and b) —Cl —CH₂CF₃ C36 (aand b) —Cl —OCF₃ C37 (a and b) —Cl —Cl C38 (a and b) —Cl —Br C39 (a andb) —Cl —I C40 (a and b) —Cl -n-butyl C41 (a and b) —Cl —CH₃ C42 (a andb) —Cl —SCF₃ C43 (a and b) —Cl —N(CH₂CH₃)₂ C44 (a and b) —Cl —OCF₂CHF₂C45 (a and b) —Cl —C(OH)(CF₃)₂ C46 (a and b) —Cl -(1,1-dimethyl-pentyl)C47 (a and b) —Cl -(1,1-dimethyl-acetic acid) ethyl ester C48 (a and b)—Cl —N-piperidinyl C49 (a and b) —F —H C50 (a and b) —F -tert-butyl C51(a and b) —F -iso-butyl C52 (a and b) —F -sec-butyl C53 (a and b) —F-iso-propyl C54 (a and b) —F -n-propyl C55 (a and b) —F -cyclohexyl C56(a and b) —F -tert-butoxy C57 (a and b) —F -isopropoxy C58 (a and b) —F—CF₃ C59 (a and b) —F —CH₂CF₃ C60 (a and b) —F —OCF₃ C61 (a and b) —F—Cl C62 (a and b) —F —Br C63 (a and b) —F —I C64 (a and b) —F -n-butylC65 (a and b) —F —CH₃ C66 (a and b) —F —SCF₃ C67 (a and b) —F—N(CH₂CH₃)₂ C68 (a and b) —F —OCF₂CHF₂ C69 (a and b) —F —C(OH)(CF₃)₂ C70(a and b) —F -(1,1-dimethyl-pentyl) C71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester C72 (a and b) —F —N-piperidinylC73 (a and b) —CH₃ —H C74 (a and b) —CH₃ -tert-butyl C75 (a and b) —CH₃-iso-butyl C76 (a and b) —CH₃ -sec-butyl C77 (a and b) —CH₃ -iso-propylC78 (a and b) —CH₃ -n-propyl C79 (a and b) —CH₃ -cyclohexyl C80 (a andb) —CH₃ -tert-butoxy C81 (a and b) —CH₃ -isopropoxy C82 (a and b) —CH₃—CF₃ C83 (a and b) —CH₃ —CH₂CF₃ C84 (a and b) —CH₃ —OCF₃ C85 (a and b)—CH₃ —Cl C86 (a and b) —CH₃ —Br C87 (a and b) —CH₃ —I C88 (a and b) —CH₃-n-butyl C89 (a and b) —CH₃ —CH₃ C90 (a and b) —CH₃ —SCF₃ C91 (a and b)—CH₃ —N(CH₂CH₃)₂ C92 (a and b) —CH₃ —OCF₂CHF₂ C93 (a and b) —CH₃—C(OH)(CF₃)₂ C94 (a and b) —CH₃ -(1,1-dimethyl-pentyl) C95 (a and b)—CH₃ -(1,1-dimethyl-acetic acid) ethyl ester C96 (a and b) —CH₃—N-piperidinyl C97 (a and b) —CF₃ —H C98 (a and b) —CF₃ -tert-butyl C99(a and b) —CF₃ -iso-butyl C100 (a and b) —CF₃ -sec-butyl C101 (a and b)—CF₃ -iso-propyl C102 (a and b) —CF₃ -n-propyl C103 (a and b) —CF₃-cyclohexyl C104 (a and b) —CF₃ -tert-butoxy C105 (a and b) —CF₃-isopropoxy C106 (a and b) —CF₃ —CF₃ C107 (a and b) —CF₃ —CH₂CF₃ C108 (aand b) —CF₃ —OCF₃ C109 (a and b) —CF₃ —Cl C110 (a and b) —CF₃ —Br C111(a and b) —CF₃ —I C112 (a and b) —CF₃ -n-butyl C113 (a and b) —CF₃ —CH₃C114 (a and b) —CF₃ —SCF₃ C115 (a and b) —CF₃ —N(CH₂CH₃)₂ C116 (a and b)—CF₃ —OCF₂CHF₂ C117 (a and b) —CF₃ —C(OH)(CF₃)₂ C118 (a and b) —CF₃-(1,1-dimethyl-pentyl) C119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester C120 (a and b) —CF₃ —N-piperidinyl C121 (a and b) —CHF₂-tert-butyl C122 (a and b) —CHF₂ —H C123 (a and b) —CHF₂ -iso-butyl C124(a and b) —CHF₂ -sec-butyl C125 (a and b) —CHF₂ -iso-propyl C126 (a andb) —CHF₂ -n-propyl C127 (a and b) —CHF₂ -cyclohexyl C128 (a and b) —CHF₂-tert-butoxy C129 (a and b) —CHF₂ -isopropoxy C130 (a and b) —CHF₂ —CF₃C131 (a and b) —CHF₂ —CH₂CF₃ C132 (a and b) —CHF₂ —OCF₃ C133 (a and b)—CHF₂ —Cl C134 (a and b) —CHF₂ —Br C135 (a and b) —CHF₂ —I C136 (a andb) —CHF₂ -n-butyl C137 (a and b) —CHF₂ —CH₃ C138 (a and b) —CHF₂ —SCF₃C139 (a and b) —CHF₂ —N(CH₂CH₃)₂ C140 (a and b) —CHF₂ —OCF₂CHF₂ C141 (aand b) —CHF₂ —C(OH)(CF₃)₂ C142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)C143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester C144 (a andb) —CHF₂ —N-piperidinyl C145 (a and b) —OH —H C146 (a and b) —OH-tert-butyl C147 (a and b) —OH -iso-butyl C148 (a and b) —OH -sec-butylC149 (a and b) —OH -iso-propyl C150 (a and b) —OH -n-propyl C151 (a andb) —OH -cyclohexyl C152 (a and b) —OH -tert-butoxy C153 (a and b) —OH-isopropoxy C154 (a and b) —OH —CF₃ C155 (a and b) —OH —CH₂CF₃ C156 (aand b) —OH —OCF₃ C157 (a and b) —OH —Cl C158 (a and b) —OH —Br C159 (aand b) —OH —I C160 (a and b) —OH -n-butyl C161 (a and b) —OH —CH₃ C162(a and b) —OH —SCF₃ C163 (a and b) —OH —N(CH₂CH₃)₂ C164 (a and b) —OH—OCF₂CHF₂ C165 (a and b) —OH —C(OH)(CF₃)₂ C166 (a and b) —OH-(1,1-dimethyl-pentyl) C167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester C168 (a and b) —OH —N-piperidinyl C169 (a and b) —NO₂ —HC170 (a and b) —NO₂ -tert-butyl C171 (a and b) —NO₂ -iso-butyl C172 (aand b) —NO₂ -sec-butyl C173 (a and b) —NO₂ -iso-propyl C174 (a and b)—NO₂ -n-propyl C175 (a and b) —NO₂ -cyclohexyl C176 (a and b) —NO₂-tert-butoxy C177 (a and b) —NO₂ -isopropoxy C178 (a and b) —NO₂ —CF₃C179 (a and b) —NO₂ —CH₂CF₃ C180 (a and b) —NO₂ —OCF₃ C181 (a and b)—NO₂ —Cl C182 (a and b) —NO₂ —Br C183 (a and b) —NO₂ —I C184 (a and b)—NO₂ -n-butyl C185 (a and b) —NO₂ —CH₃ C186 (a and b) —NO₂ —SCF₃ C187 (aand b) —NO₂ —N(CH₂CH₃)₂ C188 (a and b) —NO₂ —OCF₂CHF₂ C189 (a and b)—NO₂ —C(OH)(CF₃)₂ C190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) C191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester C192 (a and b) —NO₂—N-piperidinyl C193 (a and b) —CN —H C194 (a and b) —CN -tert-butyl C195(a and b) —CN -iso-butyl C196 (a and b) —CN -sec-butyl C197 (a and b)—CN -iso-propyl C198 (a and b) —CN -n-propyl C199 (a and b) —CN-cyclohexyl C200 (a and b) —CN -tert-butoxy C201 (a and b) —CN-isopropoxy C202 (a and b) —CN —CF₃ C203 (a and b) —CN —CH₂CF₃ C204 (aand b) —CN —OCF₃ C205 (a and b) —CN —Cl C206 (a and b) —CN —Br C207 (aand b) —CN —I C208 (a and b) —CN -n-butyl C209 (a and b) —CN —CH₃ C210(a and b) —CN —SCF₃ C211 (a and b) —CN —N(CH₂CH₃)₂ C212 (a and b) —CN—OCF₂CHF₂ C213 (a and b) —CN —C(OH)(CF₃)₂ C214 (a and b) —CN-(1,1-dimethyl-pentyl) C215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester C216 (a and b) —CN —N-piperidinyl C217 (a and b) —Br —H C218(a and b) —Br -tert-butyl C219 (a and b) —Br -iso-butyl C220 (a and b)—Br -sec-butyl C221 (a and b) —Br -iso-propyl C222 (a and b) —Br-n-propyl C223 (a and b) —Br -cyclohexyl C224 (a and b) —Br -tert-butoxyC225 (a and b) —Br -isopropoxy C226 (a and b) —Br —CF₃ C227 (a and b)—Br —CH₂CF₃ C228 (a and b) —Br —OCF₃ C229 (a and b) —Br —Cl C230 (a andb) —Br —Br C231 (a and b) —Br —I C232 (a and b) —Br -n-butyl C233 (a andb) —Br —CH₃ C234 (a and b) —Br —SCF₃ C235 (a and b) —Br —N(CH₂CH₃)₂ C236(a and b) —Br —OCF₂CHF₂ C237 (a and b) —Br —C(OH)(CF₃)₂ C238 (a and b)—Br -(1,1-dimethyl-pentyl) C239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester C240 (a and b) —Br —N-piperidinyl C241 (a and b) —I-tert-butyl C242 (a and b) —I —H C243 (a and b) —I -iso-butyl C244 (aand b) —I -sec-butyl C245 (a and b) —I -iso-propyl C246 (a and b) —I-n-propyl C247 (a and b) —I -cyclohexyl C248 (a and b) —I -tert-butoxyC249 (a and b) —I -isopropoxy C250 (a and b) —I —CF₃ C251 (a and b) —I—CH₂CF₃ C252 (a and b) —I —OCF₃ C253 (a and b) —I —Cl C254 (a and b) —I—Br C255 (a and b) —I —I C256 (a and b) —I -n-butyl C257 (a and b) —I—CH₃ C258 (a and b) —I —SCF₃ C259 (a and b) —I —N(CH₂CH₃)₂ C260 (a andb) —I —OCF₂CHF₂ C261 (a and b) —I —C(OH)(CF₃)₂ C262 (a and b) —I-(1,1-dimethyl-pentyl) C263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester C264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 4 (Id)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b) D01 (a and b) S —H —Cl —H D02 (a and b) S —H —Br —HD03 (a and b) S —H —F —H D04 (a and b) S —H —CH₃ —H D05 (a and b) S —H—CF₃ —H D06 (a and b) S —H —OCH₃ —H D07 (a and b) S —H —OCH₂CH₃ —H D08(a and b) S —H —OCF₃ —H D09 (a and b) S —H -tert-butyl —H D10 (a and b)S —H -iso-propyl —H D11 (a and b) S —H —CH₃ —CH₃ D12 (a and b) S —H —H—H D13 (a and b) S —H —H —Cl D14 (a and b) S —H —H —Br D15 (a and b) S—H —H —F D16 (a and b) S —H —H —CH₃ D17 (a and b) S —H —H —CF₃ D18 (aand b) S —H —H —OCH₃ D19 (a and b) S —H —H —OCH₂CH₃ D20 (a and b) S —H—H —OCF₃ D21 (a and b) S —H —H -tert-butyl D22 (a and b) S —H —H-iso-propyl D23 (a and b) S —Cl —Cl —H D24 (a and b) S —Cl —Br —H D25 (aand b) S —Cl —F —H D26 (a and b) S —Cl —CH₃ —H D27 (a and b) S —Cl —CF₃—H D28 (a and b) S —Cl —OCH₃ —H D29 (a and b) S —Cl —OCH₂CH₃ —H D30 (aand b) S —Cl —OCF₃ —H D31 (a and b) S —Cl -tert-butyl —H D32 (a and b) S—Cl -iso-propyl —H D33 (a and b) S —Cl —CH₃ —CH₃ D34 (a and b) S —Cl —H—H D35 (a and b) S —Cl —H —CH₃ D36 (a and b) S —Cl —H —Cl D37 (a and b)S —Cl —H —Br D38 (a and b) S —Cl —H —F D39 (a and b) S —Cl —H —CF₃ D40(a and b) S —Cl —H —OCH₃ D41 (a and b) S —Cl —H —OCH₂CH₃ D42 (a and b) S—Cl —H —OCF₃ D43 (a and b) S —Cl —H -tert-butyl D44 (a and b) S —Cl —H-iso-propyl D45 (a and b) S —Cl —H —OCF₃ D46 (a and b) S —Cl —H-tert-butyl D47 (a and b) S —Cl —H -iso-propyl D48 (a and b) S —CH₃ —Cl—H D49 (a and b) S —CH₃ —Br —H D50 (a and b) S —CH₃ —F —H D51 (a and b)S —CH₃ —CH₃ —H D52 (a and b) S —CH₃ —CF₃ —H D53 (a and b) S —CH₃ —OCH₃—H D54 (a and b) S —CH₃ —OCH₂CH₃ —H D55 (a and b) S —CH₃ —OCF₃ —H D56 (aand b) S —CH₃ -tert-butyl —H D57 (a and b) S —CH₃ -iso-propyl —H D58 (aand b) S —CH₃ —CH₃ —CH₃ D59 (a and b) S —CH₃ —H —H D60 (a and b) S —CH₃—H —Cl D61 (a and b) S —CH₃ —H —Br D62 (a and b) S —CH₃ —H —F D63 (a andb) S —CH₃ —H —CH₃ D64 (a and b) S —CH₃ —H —CF₃ D65 (a and b) S —CH₃ —H—OCH₃ D66 (a and b) S —CH₃ —H —OCH₂CH₃ D67 (a and b) S —CH₃ —H —OCF₃ D68(a and b) S —CH₃ —H -tert-butyl D69 (a and b) S —CH₃ —H -iso-propyl D70(a and b) S —CF₃ —Cl —H D71 (a and b) S —CF₃ —Br —H D72 (a and b) S —CF₃—F —H D73 (a and b) S —CF₃ —CH₃ —H D74 (a and b) S —CF₃ —CF₃ —H D75 (aand b) S —CF₃ —OCH₃ —H D76 (a and b) S —CF₃ —OCH₂CH₃ —H D77 (a and b) S—CF₃ —OCF₃ —H D78 (a and b) S —CF₃ -tert-butyl -H D79 (a and b) S —CF₃-iso-propyl -H D80 (a and b) S —CF₃ —CH₃ —CH₃ D81 (a and b) S —CF₃ —H —HD82 (a and b) S —CF₃ —H —Cl D83 (a and b) S —CF₃ —H —Br D84 (a and b) S—CF₃ —H —F D85 (a and b) S —CF₃ —H —CH₃ D86 (a and b) S —CF₃ —H —CF₃ D87(a and b) S —CF₃ —H —OCH₃ D88 (a and b) S —CF₃ —H —OCH₂CH₃ D89 (a and b)S —CF₃ —H —OCF₃ D90 (a and b) S —CF₃ —H -tert-butyl D91 (a and b) S —CF₃—H -iso-propyl D92 (a and b) S —CHF₂ —Cl —H D93 (a and b) S —CHF₂ —Br —HD94 (a and b) S —CHF₂ —F —H D95 (a and b) S —CHF₂ —CH₃ —H D96 (a and b)S —CHF₂ —CF₃ —H D97 (a and b) S —CHF₂ —OCH₃ —H D98 (a and b) S —CHF₂—OCH₂C H₃ —H D99 (a and b) S —CHF₂ —OCF₃ —H D100 (a and b) S —CHF₂-tert-butyl -H D101 (a and b) S —CHF₂ -iso-propyl -H D102 (a and b) S—CHF₂ —CH₃ —CH₃ D103 (a and b) S —CHF₂ —H —H D104 (a and b) S —CHF₂ —H—Cl D105 (a and b) S —CHF₂ —H —Br D106 (a and b) S —CHF₂ —H —F D107 (aand b) S —CHF₂ —H —CH₃ D108 (a and b) S —CHF₂ —H —CF₃ D109 (a and b) S—CHF₂ —H —OCH₃ D110 (a and b) S —CHF₂ —H —OCH₂CH₃ D111 (a and b) S —CHF₂—H —OCF₃ D112 (a and b) S —CHF₂ —H -tert-butyl D113 (a and b) S —CHF₂ —H-iso-propyl D114 (a and b) S —OH —Cl —H D115 (a and b) S —OH —Br —H D116(a and b) S —OH —F —H D117 (a and b) S —OH —CH₃ —H D118 (a and b) S —OH—CF₃ —H D119 (a and b) S —OH —OCH₃ —H D120 (a and b) S —OH —OCH₂CH₃ —HD121 (a and b) S —OH —OCF₃ —H D122 (a and b) S —OH -tert-butyl -H D123(a and b) S —OH -iso-propyl -H D124 (a and b) S —OH —CH₃ —CH₃ D125 (aand b) S —OH —H —H D126 (a and b) S —OH —H —Cl D127 (a and b) S —OH —H—Br D128 (a and b) S —OH —H —F D129 (a and b) S —OH —H —CH₃ D130 (a andb) S —OH —H —CF₃ D131 (a and b) S —OH —H —OCH₃ D132 (a and b) S —OH —H—OCH₂CH₃ D133 (a and b) S —OH —H —OCF₃ D134 (a and b) S —OH —H-tert-butyl D135 (a and b) S —OH —H -iso-propyl D136 (a and b) S —NO₂—Cl —H D137 (a and b) S —NO₂ —Br —H D138 (a and b) S —NO₂ —F —H D139 (aand b) S —NO₂ —CH₃ —H D140 (a and b) S —NO₂ —CF₃ —H D141 (a and b) S—NO₂ —OCH₃ —H D142 (a and b) S —NO₂ —OCH₂CH₃ —H D143 (a and b) S —NO₂—OCF₃ —H D144 (a and b) S —NO₂ -tert-butyl -H D145 (a and b) S —NO₂-iso-propyl -H D146 (a and b) S —NO₂ —CH₃ —CH₃ D147 (a and b) S —NO₂ —H—H D148 (a and b) S —NO₂ —H —Cl D149 (a and b) S —NO₂ —H —Br D150 (a andb) S —NO₂ —H —F D151 (a and b) S —NO₂ —H —CH₃ D152 (a and b) S —NO₂ —H—CF₃ D153 (a and b) S —NO₂ —H —OCH₃ D154 (a and b) S —NO₂ —H —OCH₂CH₃D155 (a and b) S —NO₂ —H —OCF₃ D156 (a and b) S —NO₂ —H -tert-butyl D157(a and b) S —NO₂ —H -iso-propyl D158 (a and b) S —CN —Br —H D159 (a andb) S —CN —Cl —H D160 (a and b) S —CN —F —H D161 (a and b) S —CN —CH₃ —HD162 (a and b) S —CN —CF₃ —H D163 (a and b) S —CN —OCH₃ —H D164 (a andb) S —CN —OCH₂CH₃ —H D165 (a and b) S —CN —OCF₃ —H D166 (a and b) S —CN-tert-butyl -H D167 (a and b) S —CN -iso-propyl -H D168 (a and b) S —CN—CH₃ —CH₃ D169 (a and b) S —CN —H —H D170 (a and b) S —CN —H —Cl D171 (aand b) S —CN —H —Br D172 (a and b) S —CN —H —F D173 (a and b) S —CN —H—CH₃ D174 (a and b) S —CN —H —CF₃ D175 (a and b) S —CN —H —OCH₃ D176 (aand b) S —CN —H —OCH₂CH₃ D177 (a and b) S —CN —H —OCF₃ D178 (a and b) S—CN —H -tert-butyl D179 (a and b) S —CN —H -iso-propyl D180 (a and b) S—Br —Br —H D181 (a and b) S —Br —Cl —H D182 (a and b) S —Br —H D183 (aand b) S —Br —CH₃ —H D184 (a and b) S —Br —CF₃ —H D185 (a and b) S —Br—OCH₃ —H D186 (a and b) S —Br —OCH₂CH₃ —H D187 (a and b) S —Br —OCF₃ —HD188 (a and b) S —Br -tert-butyl -H D189 (a and b) S —Br -iso-propyl -HD190 (a and b) S —Br —CH₃ —CH₃ D191 (a and b) S —Br —H —H D192 (a and b)S —Br —H —Cl D193 (a and b) S —Br —H —Br D194 (a and b) S —Br —H —F D195(a and b) S —Br —H —CH₃ D196 (a and b) S —Br —H —CF₃ D197 (a and b) S—Br —H —OCH₃ D198 (a and b) S —Br —H —OCH₂CH₃ D199 (a and b) S —Br —H—OCF₃ D200 (a and b) S —Br —H -tert-butyl D201 (a and b) S —Br —H-iso-propyl D202 (a and b) S —I —Cl —H D203 (a and b) S —I —Br —H D204(a and b) S —I —F —H D205 (a and b) S —I —CH₃ —H D206 (a and b) S —I—CF₃ —H D207 (a and b) S —I —OCH₃ —H D208 (a and b) S —I —OCH₂CH₃ —HD209 (a and b) S —I —OCF₃ —H D210 (a and b) S —I -tert-butyl —H D211 (aand b) S —I -iso-propyl —H D212 (a and b) S —I —CH₃ —CH₃ D213 (a and b)S —I —H —H D214 (a and b) S —I —H —Cl D215 (a and b) S —I —H —Br D216 (aand b) S —I —H —F D217 (a and b) S —I —H —CH₃ D218 (a and b) S —I —H—CF₃ D219 (a and b) S —I —H —OCH₃ D220 (a and b) S —I —H —OCH₂CH₃ D221(a and b) S —I —H —OCF₃ D222 (a and b) S —I —H -cert-butyl D223 (a andb) S —I —H -iso-propyl D224 (a and b) O —H —Cl —H D225 (a and b) O —H—Br —H D226 (a and b) O —H —F —H D227 (a and b) O —H —CH₃ —H D228 (a andb) O —H —CF₃ —H D229 (a and b) O —H —OCH₃ —H D230 (a and b) O —H—OCH₂CH₃ —H D231 (a and b) O —H —OCF₃ —H D232 (a and b) O —H -tert-butyl—H D233 (a and b) O —H -iso-propyl —H D234 (a and b) O —H —CH₃ —CH₃ D235(a and b) O —H —H —H D236 (a and b) O —H —H —Cl D237 (a and b) O —H —H—Br D238 (a and b) O —H —H —F D239 (a and b) O —H —H —CH₃ D240 (a and b)O —H —H —CF₃ D241 (a and b) O —H —H —OCH₃ D242 (a and b) O —H —H—OCH₂CH₃ D243 (a and b) O —H —H —OCF₃ D244 (a and b) O —H —H -tert-butylD245 (a and b) O —H —H -iso-propyl D246 (a and b) O —Cl —Cl —H D247 (aand b) O —Cl —Br —H D248 (a and b) O —Cl —F —H D249 (a and b) O —Cl —CH₃—H D250 (a and b) O —Cl —CF₃ —H D251 (a and b) O —Cl —OCH₃ —H D252 (aand b) O —Cl —OCH₂CH₃ —H D253 (a and b) O —Cl —OCF₃ —H D254 (a and b) O—Cl -tert-butyl —H D255 (a and b) O —Cl -iso-propyl —H D256 (a and b) O—Cl —CH₃ —CH₃ D257 (a and b) O —Cl —H —H D258 (a and b) O —Cl —H —CH₃D259 (a and b) O —Cl —H —Cl D260 (a and b) O —Cl —H —Br D261 (a and b) O—Cl —H —F D262 (a and b) O —Cl —H —CF₃ D263 (a and b) O —Cl —H —OCH₃D264 (a and b) O —Cl —H —OCH₂CH₃ D265 (a and b) O —Cl —H —OCF₃ D266 (aand b) O —Cl —H -tert-butyl D267 (a and b) O —Cl —H -iso-propyl D268 (aand b) O —Cl —H —OCF₃ D269 (a and b) O —Cl —H -tert-butyl D270 (a and b)O —Cl —H -iso-propyl D271 (a and b) O —CH₃ —Cl —H D272 (a and b) O —CH₃—Br —H D273 (a and b) O —CH₃ —F —H D274 (a and b) O —CH₃ —CH₃ —H D275 (aand b) O —CH₃ —CF₃ —H D276 (a and b) O —CH₃ —OCH₃ —H D277 (a and b) O—CH₃ —OCH₂CH₃ —H D278 (a and b) O —CH₃ —OCF₃ —H D279 (a and b) O —CH₃-tert-butyl —H D280 (a and b) O —CH₃ -iso-propyl —H D281 (a and b) O—CH₃ —CH₃ —CH₃ D282 (a and b) O —CH₃ —H —H D283 (a and b) O —CH₃ —H —ClD284 (a and b) O —CH₃ —H —Br D285 (a and b) O —CH₃ —H —F D286 (a and b)O —CH₃ —H —CH₃ D287 (a and b) O —CH₃ —H —CF₃ D288 (a and b) O —CH₃ —H—OCH₃ D289 (a and b) O —CH₃ —H —OCH₂CH₃ D290 (a and b) O —CH₃ —H —OCF₃D291 (a and b) O —CH₃ —H -tert-butyl D292 (a and b) O —CH₃ —H-iso-propyl D293 (a and b) O —CF₃ —Cl —H D294 (a and b) O —CF₃ —Br —HD295 (a and b) O —CF₃ —F —H D296 (a and b) O —CF₃ —CH₃ —H D297 (a and b)O —CF₃ —CF₃ —H D298 (a and b) O —CF₃ —OCH₃ —H D299 (a and b) O —CF₃—OCH₂CH₃ —H D300 (a and b) O —CF₃ —OCF₃ —H D301 (a and b) O —CF₃-tert-butyl —H D302 (a and b) O —CF₃ -iso-propyl —H D303 (a and b) O—CF₃ —CH₃ —CH₃ D304 (a and b) O —CF₃ —H —H D305 (a and b) O —CF₃ —H —ClD306 (a and b) O —CF₃ —H —Br D307 (a and b) O —CF₃ —H —F D308 (a and b)O —CF₃ —H —CH₃ D309 (a and b) O —CF₃ —H —CF₃ D310 (a and b) O —CF₃ —H—OCH₃ D311 (a and b) O —CF₃ —H —OCH₂CH₃ D312 (a and b) O —CF₃ —H —OCF₃D313 (a and b) O —CF₃ —H -tert-butyl D314 (a and b) O —CF₃ —H-iso-propyl D315 (a and b) O —CHF₂ —Cl —H D316 (a and b) O —CHF₂ —Br —HD317 (a and b) O —CHF₂ —F —H D318 (a and b) O —CHF₂ —CH₃ —H D319 (a andb) O —CHF₂ —CF₃ —H D320 (a and b) O —CHF₂ —OCH₃ —H D321 (a and b) O—CHF₂ —OCH₂CH₃ —H D322 (a and b) O —CHF₂ —OCF₃ —H D323 (a and b) O —CHF₂-tert-butyl —H D324 (a and b) O —CHF₂ -iso-propyl —H D325 (a and b) O—CHF₂ —CH₃ —CH₃ D326 (a and b) O —CHF₂ —H —H D327 (a and b) O —CHF₂ —H—Cl D328 (a and b) O —CHF₂ —H —Br D329 (a and b) O —CHF₂ —H —F D330 (aand b) O —CHF₂ —H —CH₃ D331 (a and b) O —CHF₂ —H —CF₃ D332 (a and b) O—CHF₂ —H —OCH₃ D333 (a and b) O —CHF₂ —H —OCH₂CH₃ D334 (a and b) O —CHF₂—H —OCF₃ D335 (a and b) O —CHF₂ —H -tert-butyl D336 (a and b) O —CHF₂ —H-iso-propyl D337 (a and b) O —OH —Cl —H D338 (a and b) O —OH —Br —H D339(a and b) O —OH —F —H D340 (a and b) O —OH —CH₃ —H D341 (a and b) O —OH—CF₃ —H D342 (a and b) O —OH —OCH₃ —H D343 (a and b) O —OH —OCH₂CH₃ —HD344 (a and b) O —OH —OCF₃ —H D345 (a and b) O —OH -tert-butyl —H D346(a and b) O —OH -iso-propyl —H D347 (a and b) O —OH —CH₃ —CH₃ D348 (aand b) O —OH —H —H D349 (a and b) O —OH —H —Cl D350 (a and b) O —OH —H—Br D351 (a and b) O —OH —H —F D352 (a and b) O —OH —H —CH₃ D353 (a andb) O —OH —H —CF₃ D354 (a and b) O —OH —H —OCH₃ D355 (a and b) O —OH —H—OCH₂CH₃ D356 (a and b) O —OH —H —OCF₃ D357 (a and b) O —OH —H-tert-butyl D358 (a and b) O —OH —H -iso-propyl D359 (a and b) O —NO₂—Cl —H D360 (a and b) O —NO₂ —Br —H D361 (a and b) O —NO₂ —F —H D362 (aand b) O —NO₂ —CH₃ —H D363 (a and b) O —NO₂ —CF₃ —H D364 (a and b) O—NO₂ —OCH₃ —H D365 (a and b) O —NO₂ —OCH₂CH₃ —H D366 (a and b) O —NO₂—OCF₃ —H D367 (a and b) O —NO_(2.) -tert-butyl —H D368 (a and b) O —NO₂-iso-propyl —H D369 (a and b) O —NO₂ —CH₃ —CH₃ D370 (a and b) O —NO₂ —H—H D371 (a and b) O —NO₂ —H —Cl D372 (a and b) O —NO₂ —H —Br D373 (a andb) O —NO₂ —H —F D374 (a and b) O —NO₂ —H —CH₃ D375 (a and b) O —NO₂ —H—CF₃ D376 (a and b) O —NO₂ —H —OCH₃ D377 (a and b) O —NO₂ —H —OCH₂CH₃D378 (a and b) O —NO₂ —H —OCF₃ D379 (a and b) O —NO₂ —H -tert-butyl D380(a and b) O —NO₂ —H -iso-propyl D381 (a and b) O —CN —Br —H D382 (a andb) O —CN —Cl —H D383 (a and b) O —CN —F —H D384 (a and b) O —CN —CH₃ —HD385 (a and b) O —CN —CF₃ —H D386 (a and b) O —CN —OCH₃ —H D387 (a andb) O —CN —OCH₂CH₃ —H D388 (a and b) O —CN —OCF₃ —H D389 (a and b) O —CN-tert-butyl —H D390 (a and b) O —CN -iso-propyl —H D391 (a and b) O —CN—CH₃ —CH₃ D392 (a and b) O —CN —H —H D393 (a and b) O —CN —H —Cl D394 (aand b) O —CN —H —Br D395 (a and b) O —CN —H —F D396 (a and b) O —CN —H—CH₃ D397 (a and b) O —CN —H —CF₃ D398 (a and b) O —CN —H —OCH₃ D399 (aand b) O —CN —H —OCH₂CH₃ D400 (a and b) O —CN —H —OCF₃ D401 (a and b) O—CN —H -tert-butyl D402 (a and b) O —CN —H -iso-propyl D403 (a and b) O—Br —Br —H D404 (a and b) O —Br —Cl —H D405 (a and b) O —Br —F —H D406(a and b) O —Br —CH₃ —H D407 (a and b) O —Br —CF₃ —H D408 (a and b) O—Br —OCH₃ —H D409 (a and b) O —Br —OCH₂CH₃ —H D410 (a and b) O —Br —OCF₃—H D411 (a and b) O —Br -tert-butyl —H D412 (a and b) O —Br -iso-propyl—H D413 (a and b) O —Br —CH₃ —CH₃ D414 (a and b) O —Br —H —H D415 (a andb) O —Br —H —Cl D416 (a and b) O —Br —H —Br D417 (a and b) O —Br —H —FD418 (a and b) O —Br —H —CH₃ D419 (a and b) O —Br —H —CF₃ D420 (a and b)O —Br —H —OCH₃ D421 (a and b) O —Br —H —OCH₂CH₃ D422 (a and b) O —Br —H—OCF₃ D423 (a and b) O —Br —H -tert-butyl D424 (a and b) O —Br —H-iso-propyl D425 (a and b) O —I —Cl —H D426 (a and b) O —I —Br —H D427(a and b) O —I —F —H D428 (a and b) O —I —CH₃ —H D429 (a and b) O —I—CF₃ —H D430 (a and b) O —I —OCH₃ —H D431 (a and b) O —I —OCH₂CH₃ —HD432 (a and b) O —I —OCF₃ —H D433 (a and b) O —I -tert-butyl —H D434 (aand b) O —I -iso-propyl —H D435 (a and b) O —I —CH₃ —CH₃ D436 (a and b)O —I —H —H D437 (a and b) O —I —H —Cl D438 (a and b) O —I —H —Br D439 (aand b) O —I —H —F D440 (a and b) O —I —H —CH₃ D441 (a and b) O —I —H—OCF₃ D442 (a and b) O —I —H —OCH₃ D443 (a and b) O —I —H —OCH₂CH₃ D444(a and b) O —I —H —OCF₃ D445 (a and b) O —I —H -tert-butyl D446 (a andb) O —I —H -iso-propyl D447 (a and b) NH —H —Cl —H D448 (a and b) NH —H—Br —H D449 (a and b) NH —H —F —H D450 (a and b) NH —H —CH₃ —H D451 (aand b) NH —H —CF₃ —H D452 (a and b) NH —H —OCH₃ —H D453 (a and b) NH —H—OCH₂CH₃ —H D454 (a and b) NH —H —OCF₃ —H D455 (a and b) NH —H-tert-butyl —H D456 (a and b) NH —H -iso-propyl —H D457 (a and b) NH —H—CH₃ —CH₃ D458 (a and b) NH —H —H —H D459 (a and b) NH —H —H —Cl D460 (aand b) NH —H —H —Br D461 (a and b) NH —H —H —F D462 (a and b) NH —H —H—CH₃ D463 (a and b) NH —H —H —CF₃ D464 (a and b) NH —H —H —OCH₃ D465 (aand b) NH —H —H —OCH₂CH₃ D466 (a and b) NH —H —H —OCF₃ D467 (a and b) NH—H —H -tert-butyl D468 (a and b) NH —H —H -iso-propyl D469 (a and b) NH—Cl —Cl —H D470 (a and b) NH —Cl —Br —H D471 (a and b) NH —Cl —F —H D472(a and b) NH —Cl —CH₃ —H D473 (a and b) NH —Cl —CF₃ —H D474 (a and b) NH—Cl —OCH₃ —H D475 (a and b) NH —Cl —OCH₂CH₃ —H D476 (a and b) NH —Cl—OCF₃ —H D477 (a and b) NH —Cl -tert-butyl —H D478 (a and b) NH —Cl-iso-propyl —H D479 (a and b) NH —Cl —CH₃ —CH₃ D480 (a and b) NH —Cl —H—H D481 (a and b) NH —Cl —H —Cl D482 (a and b) NH —Cl —H —Br D483 (a andb) NH —Cl —H —F D484 (a and b) NH —Cl —H —CH₃ D485 (a and b) NH —Cl —H—CF₃ D486 (a and b) NH —Cl —H —OCH₃ D487 (a and b) NH —Cl —H —OCH₂CH₃D488 (a and b) NH —Cl —H —OCF₃ D489 (a and b) NH —Cl —H -tert-butyl D490(a and b) NH —Cl —H -iso-propyl D491 (a and b) NH —Cl —H —OCF₃ D492 (aand b) NH —Cl —H -tert-butyl D493 (a and b) NH —Cl —H -iso-propyl D494(a and b) NH —CH₃ —Cl —H D495 (a and b) NH —CH₃ —Br —H D496 (a and b) NH—CH₃ —F —H D497 (a and b) NH —CH₃ —CH₃ —H D498 (a and b) NH —CH₃ —CF₃ —HD499 (a and b) NH —CH₃ —OCH₃ —H D500 (a and b) NH —CH₃ —OCH₂CH₃ —H D501(a and b) NH —CH₃ —OCF₃ —H D502 (a and b) NH —CH₃ -tert-butyl —H D503 (aand b) NH —CH₃ -iso-propyl —H D504 (a and b) NH —CH₃ —CH₃ —CH₃ D505 (aand b) NH —CH₃ —H —H D506 (a and b) NH —CH₃ —H —Cl D507 (a and b) NH—CH₃ —H —Br D508 (a and b) NH —CH₃ —H —F D509 (a and b) NH —CH₃ —H —CH₃D510 (a and b) NH —CH₃ —H —CF₃ D511 (a and b) NH —CH₃ —H —OCH₃ D512 (aand b) NH —CH₃ —H —OCH₂CH₃ D513 (a and b) NH —CH₃ —H —OCF₃ D514 (a andb) NH —CH₃ —H -tert-butyl D515 (a and b) NH —CH₃ —H -iso-propyl D516 (aand b) NH —CF₃ —Cl —H D517 (a and b) NH —CF₃ —Br —H D518 (a and b) NH—CF₃ —F —H D519 (a and b) NH —CF₃ —CH₃ —H D520 (a and b) NH —CF₃ —CF₃ —HD521 (a and b) NH —CF₃ —OCH₃ —H D522 (a and b) NH —CF₃ —OCH₂CH₃ —H D523(a and b) NH —CF₃ —OCF₃ —H D524 (a and b) NH —CF₃ -tert-butyl —H D525 (aand b) NH —CF₃ -iso-propyl —H D526 (a and b) NH —CF₃ —CH₃ —CH₃ D527 (aand b) NH —CF₃ —H —H D528 (a and b) NH —CF₃ —H —Cl D529 (a and b) NH—CF₃ —H —Br D530 (a and b) NH —CF₃ —H —F D531 (a and b) NH —CF₃ —H —CH₃D532 (a and b) NH —CF₃ —H —CF₃ D533 (a and b) NH —CF₃ —H —OCH₃ D534 (aand b) NH —CF₃ —H —OCH₂CH₃ D535 (a and b) NH —CF₃ —H —OCF₃ D536 (a andb) NH —CF₃ —H -tert-butyl D537 (a and b) NH —CF₃ —H -iso-propyl D538 (aand b) NH —CHF₂ —Cl —H D539 (a and b) NH —CHF₂ —Br —H D540 (a and b) NH—CHF₂ —F —H D541 (a and b) NH —CHF₂ —CH₃ —H D542 (a and b) NH —CHF₂ —CF₃—H D543 (a and b) NH —CHF₂ —OCH₃ —H D544 (a and b) NH —CHF₂ —OCH₂CH₃ —HD545 (a and b) NH —CHF₂ —OCF₃ —H D546 (a and b) NH —CHF₂ -tert-butyl —HD547 (a and b) NH —CHF₂ -iso-propyl —H D548 (a and b) NH —CHF₂ —CH₃ —CH₃D549 (a and b) NH —CHF₂ —H —H D550 (a and b) NH —CHF₂ —H —Cl D551 (a andb) NH —CHF₂ —H —Br D552 (a and b) NH —CHF₂ —H —F D553 (a and b) NH —CHF₂—H —CH₃ D554 (a and b) NH —CHF₂ —H —CF₃ D555 (a and b) NH —CHF₂ —H —OCH₃D556 (a and b) NH —CHF₂ —H —OCH₂CH₃ D557 (a and b) NH —CHF₂ —H —OCF₃D558 (a and b) NH —CHF₂ —H -tert-butyl D559 (a and b) NH —CHF₂ —H-iso-propyl D560 (a and b) NH —OH —C1 —H D561 (a and b) NH —OH —Br —HD562 (a and b) NH —OH —F —H D563 (a and b) NH —OH —CH₃ —H D564 (a and b)NH —OH —CF₃ —H D565 (a and b) NH —OH —OCH₃ —H D566 (a and b) NH —OH—OCH₂CH₃ —H D567 (a and b) NH —OH —OCF₃ —H D568 (a and b) NH —OH-tert-butyl —H D569 (a and b) NH —OH -iso-propyl —H D570 (a and b) NH—OH —CH₃ —CH₃ D571 (a and b) NH —OH —H —H D572 (a and b) NH —OH —H —ClD573 (a and b) NH —OH —H —Br D574 (a and b) NH —OH —H —F D575 (a and b)NH —OH —H —CH₃ D576 (a and b) NH —OH —H —CF₃ D577 (a and b) NH —OH —H—OCH₃ D578 (a and b) NH —OH —H —OCH₂CH₃ D579 (a and b) NH —OH —H —OCF₃D580 (a and b) NH —OH —H -tert-butyl D581 (a and b) NH —OH —H-iso-propyl D582 (a and b) NH —NO₂ —C1 —H D583 (a and b) NH —NO₂ —Br —HD584 (a and b) NH —NO₂ —F —H D585 (a and b) NH —NO₂ —CH₃ —H D586 (a andb) NH —NO₂ —CF₃ —H D587 (a and b) NH —NO₂ —OCH₃ —H D588 (a and b) NH—NO₂ —OCH₂CH₃ —H D589 (a and b) NH —NO₂ —OCF₃ —H D590 (a and b) NH —NO₂-tert-butyl —H DS91 (a and b) NH —NO₂ -iso-propyl —H D592 (a and b) NH—NO₂ —CH₃ —CH₃ D593 (a and b) NH —NO₂ —H —H D594 (a and b) NH —NO₂ —H—Cl D595 (a and b) NH —NO₂ —H —Br D596 (a and b) NH —NO₂ —H —F D597 (aand b) NH —NO₂ —H —CH₃ D598 (a and b) NH —NO₂ —H —CF₃ D599 (a and b) NH—NO₂ —H —OCH₃ D600 (a and b) NH —NO₂ —H —OCH₂CH₃ D601 (a and b) NH —NO₂—H —OCF₃ D602 (a and b) NH —NO₂ —H -tert-butyl D603 (a and b) NH —NO₂ —H-iso-propyl D604 (a and b) NH —CN —Br —H D605 (a and b) NH —CN —Cl —HD606 (a and b) NH —CN —F —H D607 (a and b) NH —CN —CH₃ —H D608 (a and b)NH —CN —CF₃ —H D609 (a and b) NH —CN —OCH₃ —H D610 (a and b) NH —CN—OCH₂CH₃ —H D611 (a and b) NH —CN —OCF₃ —H D612 (a and b) NH —CN-tert-butyl —H D613 (a and b) NH —CN -iso-propyl —H D614 (a and b) NH—CN —CH₃ —CH₃ D615 (a and b) NH —CN —H —H D616 (a and b) NH —CN —H —ClD617 (a and b) NH —CN —H —Br D618 (a and b) NH —CN —H —F D619 (a and b)NH —CN —H —CH₃ D620 (a and b) NH —CN —H —CF₃ D621 (a and b) NH —CN —H—OCH₃ D622 (a and b) NH —CN —H —OCH₂CH₃ D623 (a and b) NH —CN —H —OCF₃D624 (a and b) NH —CN —H -tert-butyl D625 (a and b) NH —CN —H-iso-propyl D626 (a and b) NH —Br —Br —H D627 (a and b) NH —Br —Cl —HD628 (a and b) NH —Br —F —H D629 (a and b) NH —Br —CH₃ —H D630 (a and b)NH —Br —CF₃ —H D631 (a and b) NH —Br —OCH₃ —H D632 (a and b) NH —Br—OCH₂CH₃ —H D633 (a and b) NH —Br —OCF₃ —H D634 (a and b) NH —Br-tert-butyl —H D635 (a and b) NH —Br -iso-propyl —H D636 (a and b) NH—Br —CH₃ —CH₃ D637 (a and b) NH —Br —H —H D638 (a and b) NH —Br —H —ClD639 (a and b) NH —Br —H —Br D640 (a and b) NH —Br —H —F D641 (a and b)NH —Br —H —CH₃ D642 (a and b) NH —Br —H —CF₃ D643 (a and b) NH —Br —H—OCH₃ D644 (a and b) NH —Br —H —OCH₂CH₃ D645 (a and b) NH —Br —H —OCF₃D646 (a and b) NH —Br —H -tert-butyl D647 (a and b) NH —Br —H-iso-propyl D648 (a and b) NH —I —Cl —H D649 (a and b) NH —I —Br —H D650(a and b) NH —I —F —H D651 (a and b) NH —I —CH₃ —H D652 (a and b) NH —I—CF₃ —H D653 (a and b) NH —I —OCH₃ —H D654 (a and b) NH —I —OCH₂CH₃ —HD655 (a and b) NH —I —OCF₃ —H D656 (a and b) NH —I -tert-butyl —H D657(a and b) NH —I -iso-propyl —H D658 (a and b) NH —I —CH₃ —CH₃ D659 (aand b) NH —I —H —H D660 (a and b) NH —I —H —Cl D661 (a and b) NH —I —H—Br D662 (a and b) NH —I —H —F D663 (a and b) NH —I —H —CH₃ D664 (a andb) NH —I —H —CF₃ D665 (a and b) NH —I —H —OCH₃ D666 (a and b) NH —I —H—OCH₂CH₃ D667 (a and b) NH —I —H —OCF₃ D668 (a and b) NH —I —H-tert-butyl D669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 5 (Ie)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a) E01 (a and b) —H —H E02 (a and b) —H -tert-butyl E03 (a and b) —H-iso-butyl E04 (a and b) —H -sec-butyl E05 (a and b) —H -iso-propyl E06(a and b) —H -n-propyl E07 (a and b) —H -cyclohexyl E08 (a and b) —H-tert-butoxy E09 (a and b) —H -isopropoxy E10 (a and b) —H —CF₃ E11 (aand b) —H —CH₂CF₃ E12 (a and b) —H —OCF₃ E13 (a and b) —H —Cl E14 (a andb) —H —Br E15 (a and b) —H —I E16 (a and b) —H -n-butyl E17 (a and b) —H—CH₃ E18 (a and b) —H —SCF₃ E19 (a and b) —H —N(CH₂CH₃)₂ E20 (a and b)—H —OCF₂CHF₂ E21 (a and b) —H —C(OH)(CF₃)₂ E22 (a and b) —H-(1,1-dimethyl-pentyl) E23 (a and b) —H -(1,1-dimethyl-acetic acid)ethyl ester E24 (a and b) —H —N-piperidinyl E25 (a and b) —Cl —H E26 (aand b) —Cl -tert-butyl E27 (a and b) —Cl -iso-butyl E28 (a and b) —Cl-sec-butyl E29 (a and b) —Cl -iso-propyl E30 (a and b) —Cl -n-propyl E31(a and b) —Cl -cyclohexyl E32 (a and b) —Cl -tert-butoxy E33 (a and b)—Cl -isopropoxy E34 (a and b) —Cl —CF₃ E35 (a and b) —Cl —CH₂CF₃ E36 (aand b) —Cl —OCF₃ E37 (a and b) —Cl —Cl E38 (a and b) —Cl —Br E39 (a andb) —Cl —I E40 (a and b) —Cl -n-butyl E41 (a and b) —Cl —CH₃ E42 (a andb) —Cl —SCF₃ E43 (a and b) —Cl —N(CH₂CH₃)₂ E44 (a and b) —Cl —OCF₂CHF₂E45 (a and b) —Cl —C(OH)(CF₃)₂ E46 (a and b) —Cl -(1,1-dimethyl-pentyl)E47 (a and b) —Cl -(1,1-dimethyl-acetic acid) ethyl ester E48 (a and b)—Cl —N-piperidinyl E49 (a and b) —F —H E50 (a and b) —F -tert-butyl E51(a and b) —F -iso-butyl E52 (a and b) —F -sec-butyl E53 (a and b) —F-iso-propyl E54 (a and b) —F -n-propyl E55 (a and b) —F -cyclohexyl E56(a and b) —F -tert-butoxy E57 (a and b) —F -isopropoxy E58 (a and b) —F—CF₃ E59 (a and b) —F —CH₂CF₃ E60 (a and b) —F —OCF₃ E61 (a and b) —F—Cl E62 (a and b) —F —Br E63 (a and b) —F —I E64 (a and b) —F -n-butylE65 (a and b) —F —CH₃ E66 (a and b) —F —SCF₃ E67 (a and b) —F—N(CH₂CH₃)₂ E68 (a and b) —F —OCF₂CHF₂ E69 (a and b) —F —C(OH)(CF₃)₂ E70(a and b) —F -(1,1-dimethyl-pentyl) E71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester E72 (a and b) —F —N-piperidinylE73 (a and b) —CH₃ —H E74 (a and b) —CH₃ -iso-butyl E75 (a and b) —CH₃-tert-butyl E76 (a and b) —CH₃ -sec-butyl E77 (a and b) —CH₃ -iso-propylE78 (a and b) —CH₃ -n-propyl E79 (a and b) —CH₃ -cyclohexyl E80 (a andb) —CH₃ -tert-butoxy E81 (a and b) —CH₃ -isopropoxy E82 (a and b) —CH₃—CF₃ E83 (a and b) —CH₃ —CH₂CF₃ E84 (a and b) —CH₃ —OCF₃ E85 (a and b)—CH₃ —Cl E86 (a and b) —CH₃ —Br E87 (a and b) —CH₃ —I E88 (a and b) —CH₃-n-butyl E89 (a and b) —CH₃ —CH₃ E90 (a and b) —CH₃ —SCF₃ E91 (a and b)—CH₃ —N(CH₂CH₃)₂ E92 (a and b) —CH₃ —OCF₂CHF₂ E93 (a and b) —CH₃—C(OH)(CF₃)₂ E94 (a and b) —CH₃ -(1,1-dimethyl-pentyl) E95 (a and b)—CH₃ -(1,1-dimethyl-acetic acid) ethyl ester E96 (a and b) —CH₃—N-piperidinyl E97 (a and b) —CF₃ —H E98 (a and b) —CF₃ -tert-butyl E99(a and b) —CF₃ -iso-butyl E100 (a and b) —CF₃ -sec-butyl E101 (a and b)—CF₃ -iso-propyl E102 (a and b) —CF₃ -n-propyl E103 (a and b) —CF₃-cyclohexyl E104 (a and b) —CF₃ -tert-butoxy E105 (a and b) —CF₃-isopropoxy E106 (a and b) —CF₃ —CF₃ E107 (a and b) —CF₃ —CH₂CF₃ E108 (aand b) —CF₃ —OCF₃ E109 (a and b) —CF₃ —Cl E110 (a and b) —CF₃ —Br E111(a and b) —CF₃ —I E112 (a and b) —CF₃ -n-butyl E113 (a and b) —CF₃ —CH₃E114 (a and b) —CF₃ —SCF₃ E115 (a and b) —CF₃ —N(CH₂CH₃)₂ E116 (a and b)—CF₃ —OCF₂CHF₂ E117 (a and b) —CF₃ —C(OH)(CF₃)₂ E118 (a and b) —CF₃-(1,1-dimethyl-pentyl) E119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester E120 (a and b) —CF₃ —N-piperidinyl E121 (a and b) —CHF₂-tert-butyl E122 (a and b) —CHF₂ —H E123 (a and b) —CHF₂ -iso-butyl E124(a and b) —CHF₂ -sec-butyl E125 (a and b) —CHF₂ -iso-propyl E126 (a andb) —CHF₂ -n-propyl E127 (a and b) —CHF₂ -cyclohexyl E128 (a and b) —CHF₂-tert-butoxy E129 (a and b) —CHF₂ -isopropoxy E130 (a and b) —CHF₂ —CF₃E131 (a and b) —CHF₂ —CH₂CF₃ E132 (a and b) —CHF₂ —OCF₃ E133 (a and b)—CHF₂ —Cl E134 (a and b) —CHF₂ —Br E135 (a and b) —CHF₂ —I E136 (a andb) —CHF₂ -n-butyl E137 (a and b) —CHF₂ —CH₃ E138 (a and b) —CHF₂ —SCF₃E139 (a and b) —CHF₂ —N(CH₂CH₃)₂ E140 (a and b) —CHF₂ —OCF₂CHF₂ E141 (aand b) —CHF₂ —C(OH)(CF₃)₂ E142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)E143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester E144 (a andb) —CHF₂ —N-piperidinyl E145 (a and b) —OH —H E146 (a and b) —OH-tert-butyl E147 (a and b) —OH -iso-butyl E148 (a and b) —OH -sec-butylE149 (a and b) —OH -iso-propyl E150 (a and b) —OH -n-propyl E151 (a andb) —OH -cyclohexyl E152 (a and b) —OH -tert-butoxy E153 (a and b) —OH-isopropoxy E154 (a and b) —OH —CF₃ E155 (a and b) —OH —CH₂CF₃ E156 (aand b) —OH —OCF₃ E157 (a and b) —OH —Cl E158 (a and b) —OH —Br E159 (aand b) —OH —I E160 (a and b) —OH -n-butyl E161 (a and b) —OH —CH₃ E162(a and b) —OH —SCF₃ E163 (a and b) —OH —N(CH₂CH₃)₂ E164 (a and b) —OH—OCF₂CHF₂ E165 (a and b) —OH —C(OH)(CF₃)₂ E166 (a and b) —OH-(1,1-dimethyl-pentyl) E167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester E168 (a and b) —OH —N-piperidinyl E169 (a and b) —NO₂ —HE170 (a and b) —NO₂ -tert-butyl E171 (a and b) —NO₂ -iso-butyl E172 (aand b) —NO₂ -sec-butyl E173 (a and b) —NO₂ -iso-propyl E174 (a and b)—NO₂ -n-propyl E175 (a and b) —NO₂ -cyclohexyl E176 (a and b) —NO₂-tert-butoxy E177 (a and b) —NO₂ -isopropoxy E178 (a and b) —NO₂ —CF₃E179 (a and b) —NO₂ —CH₂CF₃ E180 (a and b) —NO₂ —OCF₃ E181 (a and b)—NO₂ —Cl E182 (a and b) —NO₂ —Br E183 (a and b) —NO₂ —I E184 (a and b)—NO₂ -n-butyl E185 (a and b) —NO₂ —CH₃ E186 (a and b) —NO₂ —SCF₃ E187 (aand b) —NO₂ —N(CH₂CH₃)₂ E188 (a and b) —NO₂ —OCF₂CHF₂ E189 (a and b)—NO₂ —C(OH)(CF₃)₂ E190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) E191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester E192 (a and b) —NO₂—N-piperidinyl E193 (a and b) —CN —H E194 (a and b) —CN -tert-butyl E195(a and b) —CN -iso-butyl E196 (a and b) —CN -sec-butyl E197 (a and b)—CN -iso-propyl E198 (a and b) —CN -n-propyl E199 (a and b) —CN-cyclohexyl E200 (a and b) —CN -tert-butoxy E201 (a and b) —CN-isopropoxy E202 (a and b) —CN —CF₃ E203 (a and b) —CN —CH₂CF₃ E204 (aand b) —CN —OCF₃ E205 (a and b) —CN —Cl E206 (a and b) —CN —Br E207 (aand b) —CN —I E208 (a and b) —CN -n-butyl E209 (a and b) —CN —CH₃ E210(a and b) —CN —SCF₃ E211 (a and b) —CN —N(CH₂CH₃)₂ E212 (a and b) —CN—OCF₂CHF₂ E213 (a and b) —CN —C(OH)(CF₃)₂ E214 (a and b) —CN-(1,1-dimethyl-pentyl) E215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester E216 (a and b) —CN —N-piperidinyl E217 (a and b) —Br —H E218(a and b) —Br -tert-butyl E219 (a and b) —Br -iso-butyl E220 (a and b)—Br -sec-butyl E221 (a and b) —Br -iso-propyl E222 (a and b) —Br-n-propyl E223 (a and b) —Br -cyclohexyl E224 (a and b) —Br -tert-butoxyE225 (a and b) —Br -isopropoxy E226 (a and b) —Br —CF₃ E227 (a and b)—Br —CH₂CF₃ E228 (a and b) —Br —OCF₃ E229 (a and b) —Br —Cl E230 (a andb) —Br —Br E231 (a and b) —Br —I E232 (a and b) —Br -n-butyl E233 (a andb) —Br —CH₃ E234 (a and b) —Br —SCF₃ E235 (a and b) —Br —N(CH₂CH₃)₂ E236(a and b) —Br —OCF₂CHF₂ E237 (a and b) —Br —C(OH)(CF₃)₂ E238 (a and b)—Br -(1,1-dimethyl-pentyl) E239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester E240 (a and b) —Br —N-piperidinyl E241 (a and b) —I-tert-butyl E242 (a and b) —I —H E243 (a and b) —I -iso-butyl E244 (aand b) —I -sec-butyl E245 (a and b) —I -iso-propyl E246 (a and b) —I-n-propyl E247 (a and b) —I -cyclohexyl E248 (a and b) —I -tert-butoxyE249 (a and b) —I -isopropoxy E250 (a and b) —I —CF₃ E251 (a and b) —I—CH₂CF₃ E252 (a and b) —I —OCF₃ E253 (a and b) —I —Cl E254 (a and b) —I—Br E255 (a and b) —I —I E256 (a and b) —I -n-butyl E257 (a and b) —I—CH₃ E258 (a and b) —I —SCF₃ E259 (a and b) —I —N(CH₂CH₃)₂ E260 (a andb) —I —OCF₂CHF₂ E261 (a and b) —I —C(OH)(CF₃)₂ E262 (a and b) —I-(1,1-dimethyl-pentyl) E263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester E264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 6 (If)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b) F01 (a and b) S —H —Cl —H F02 (a and b) S —H —Br —HF03 (a and b) S —H —F —H F04 (a and b) S —H —CH₃ —H F05 (a and b) S —H—CF₃ —H F06 (a and b) S —H —OCH₃ —H F07 (a and b) S —H —OCH₂CH₃ —H F08(a and b) S —H —OCF₃ —H F09 (a and b) S —H -tert-butyl —H F10 (a and b)S —H -iso-propyl —H F11 (a and b) S —H —CH₃ —CH₃ F12 (a and b) S —H —H—H F13 (a and b) S —H —H —Cl F14 (a and b) S —H —H —Br F15 (a and b) S—H —H —F F16 (a and b) S —H —H —CH₃ F17 (a and b) S —H —H —CF₃ F18 (aand b) S —H —H —OCH₃ F19 (a and b) S —H —H —OCH₂CH₃ F20 (a and b) S —H—H —OCF₃ F21 (a and b) S —H —H -tert-butyl F22 (a and b) S —H —H-iso-propyl F23 (a and b) S —Cl —Cl —H F24 (a and b) S —Cl —Br —H F25 (aand b) S —Cl —F —H F26 (a and b) S —Cl —CH₃ —H F27 (a and b) S —Cl —CF₃—H F28 (a and b) S —Cl —OCH₃ —H F29 (a and b) S —Cl —OCH₂CH₃ —H F30 (aand b) S —Cl —OCF₃ —H F31 (a and b) S —Cl -tert-butyl —H F32 (a and b) S—Cl -iso-propyl —H F33 (a and b) S —Cl —CH₃ —CH₃ F34 (a and b) S —Cl —H—H F35 (a and b) S —Cl —H —Cl F36 (a and b) S —Cl —H —Br F37 (a and b) S—Cl —H —F F38 (a and b) S —Cl —H —CH₃ F39 (a and b) S —Cl —H —CF₃ F40 (aand b) S —Cl —H —OCH₃ F41 (a and b) S —Cl —H —OCH₂CH₃ F42 (a and b) S—Cl —H —OCF₃ F43 (a and b) S —Cl —H -tert-butyl F44 (a and b) S —Cl —H-iso-propyl F45 (a and b) S —Cl —H —OCF₃ F46 (a and b) S —Cl —H-tert-butyl F47 (a and b) S —Cl —H -iso-propyl F48 (a and b) S —CH₃ —Cl—H F49 (a and b) S —CH₃ —Br —H F50 (a and b) S —CH₃ —F —H F51 (a and b)S —CH₃ —CH₃ —H F52 (a and b) S —CH₃ —CF₃ —H F53 (a and b) S —CH₃ —OCH₃—H F54 (a and b) S —CH₃ —OCH₂CH₃ —H F55 (a and b) S —CH₃ —OCF₃ —H F56 (aand b) S —CH₃ -tert-butyl —H F57 (a and b) S —CH₃ -iso-propyl —H F58 (aand b) S —CH₃ —CH₃ —CH₃ F59 (a and b) S —CH₃ —H —H F60 (a and b) S —CH₃—H —Cl F61 (a and b) S —CH₃ —H —Br F62 (a and b) S —CH₃ —H —F F63 (a andb) S —CH₃ —H —CH₃ F64 (a and b) S —CH₃ —H —CF₃ F65 (a and b) S —CH₃ —H—OCH₃ F66 (a and b) S —CH₃ —H —OCH₂CH₃ F67 (a and b) S —CH₃ —H —OCF₃ F68(a and b) S —CH₃ —H -tert-butyl F69 (a and b) S —CH₃ —H -iso-propyl F70(a and b) S —CF₃ —Cl —H F71 (a and b) S —CF₃ —Br —H F72 (a and b) S —CF₃—F —H F73 (a and b) S —CF₃ —CH₃ —H F74 (a and b) S —CF₃ —CF₃ —H F75 (aand b) S —CF₃ —OCH₃ —H F76 (a and b) S —CF₃ —OCH₂CH₃ —H F77 (a and b) S—CF₃ —OCF₃ —H F78 (a and b) S —CF₃ -tert-butyl —H F79 (a and b) S —CF₃-iso-propyl —H F80 (a and b) S —CF₃ —CH₃ —CH₃ F81 (a and b) S —CF₃ —H —HF82 (a and b) S —CF₃ —H —Cl F83 (a and b) S —CF₃ —H —Br F84 (a and b) S—CF₃ —H —F F85 (a and b) S —CF₃ —H —CH₃ F86 (a and b) S —CF₃ —H —CF₃ F87(a and b) S —CF₃ —H —OCH₃ F88 (a and b) S —CF₃ —H —OCH₂CH₃ F89 (a and b)S —CF₃ —H —OCF₃ F90 (a and b) S —CF₃ —H -tert-butyl F91 (a and b) S —CF₃—H -iso-propyl F92 (a and b) S —CHF₂ —Cl —H F93 (a and b) S —CHF₂ —Br —HF94 (a and b) S —CHF₂ —F —H F95 (a and b) S —CHF₂ —CH₃ —H F96 (a and b)S —CHF₂ —CF₃ —H F97 (a and b) S —CHF₂ —OCH₃ —H F98 (a and b) S —CHF₂—OCH₂CH₃ —H F99 (a and b) S —CHF₂ —OCF₃ —H F100 (a and b) S —CHF₂-tert-butyl —H F101 (a and b) S —CHF₂ -iso-propyl —H F102 (a and b) S—CHF₂ —CH₃ —CH₃ F103 (a and b) S —CHF₂ —H —H F104 (a and b) S —CHF₂ —H—Cl F105 (a and b) S —CHF₂ —H —Br F106 (a and b) S —CHF₂ —H —F F107 (aand b) S —CHF₂ —H —CH₃ F108 (a and b) S —CHF₂ —H —CF₃ F109 (a and b) S—CHF₂ —H —OCH₃ F110 (a and b) S —CHF₂ —H —OCH₂CH₃ F111 (a and b) S —CHF₂—H —OCF₃ F112 (a and b) S —CHF₂ —H -tert-butyl F113 (a and b) S —CHF₂ —H-iso-propyl F114 (a and b) S —OH —Cl —H F115 (a and b) S —OH —Br —H F116(a and b) S —OH —F —H F117 (a and b) S —OH —CH₃ —H F118 (a and b) S —OH—CF₃ —H F119 (a and b) S —OH —OCH₃ —H F120 (a and b) S —OH —OCH₂CH₃ —HF121 (a and b) S —OH —OCF₃ —H F122 (a and b) S —OH -tert-butyl —H F123(a and b) S —OH -iso-propyl —H F124 (a and b) S —OH —CH₃ —CH₃ F125 (aand b) S —OH —H —H F126 (a and b) S —OH —H —Cl F127 (a and b) S —OH —H—Br F128 (a and b) S —OH —H —F F129 (a and b) S —OH —H —CH₃ F130 (a andb) S —OH —H —CF₃ F131 (a and b) S —OH —H —OCH₃ F132 (a and b) S —OH —H—OCH₂CH₃ F133 (a and b) S —OH —H —OCF₃ F134 (a and b) S —OH —H-tert-butyl F135 (a and b) S —OH —H -iso-propyl F136 (a and b) S —NO₂—Cl —H F137 (a and b) S —NO₂ —Br —H F138 (a and b) S —NO₂ —F —H F139 (aand b) S —NO₂ —CH₃ —H F140 (a and b) S —NO₂ —CF₃ —H F141 (a and b) S—NO₂ —OCH₃ —H F142 (a and b) S —NO₂ —OCH₂CH₃ —H F143 (a and b) S —NO₂—OCF₃ —H F144 (a and b) S —NO₂ -tert-butyl —H F145 (a and b) S —NO₂-iso-propyl —H F146 (a and b) S —NO₂ —CH₃ —CH₃ F147 (a and b) S —NO₂ —H—H F148 (a and b) S —NO₂ —H —Cl F149 (a and b) S —NO₂ —H —Br F150 (a andb) S —NO₂ —H —F F151 (a and b) S —NO₂ —H —CH₃ F152 (a and b) S —NO₂ —H—CF₃ F153 (a and b) S —NO₂ —H —OCH₃ F154 (a and b) S —NO₂ —H —OCH₂CH₃F155 (a and b) S —NO₂ —H —OCF₃ F156 (a and b) S —NO₂ —H -tert-butyl F157(a and b) S —NO₂ —H -iso-propyl F158 (a and b) S —CN —Br —H F159 (a andb) S —CN —Cl —H F160 (a and b) S —CN —F —H F161 (a and b) S —CN —CH₃ —HF162 (a and b) S —CN —CF₃ —H F163 (a and b) S —CN —OCH₃ —H F164 (a andb) S —CN —OCH₂CH₃ —H F165 (a and b) S —CN —OCF₃ —H F166 (a and b) S —CN-tert-butyl —H F167 (a and b) S —CN -iso-propyl —H F168 (a and b) S —CN—CH₃ —CH₃ F169 (a and b) S —CN —H —H F170 (a and b) S —CN —H —Cl F171 (aand b) S —CN —H —Br F172 (a and b) S —CN —H —F F173 (a and b) S —CN —H—CH₃ F174 (a and b) S —CN —H —CF₃ F175 (a and b) S —CN —H —OCH₃ F176 (aand b) S —CN —H —OCH₂CH₃ F177 (a and b) S —CN —H —OCF₃ F178 (a and b) S—CN —H -tert-butyl F179 (a and b) S —CN —H -iso-propyl F180 (a and b) S—Br —Br —H F181 (a and b) S —Br —Cl —H F182 (a and b) S —Br —F —H F183(a and b) S —Br —CH₃ —H F184 (a and b) S —Br —CF₃ —H F185 (a and b) S—Br —OCH₃ —H F186 (a and b) S —Br —OCH₂CH₃ —H F187 (a and b) S —Br —OCF₃—H F188 (a and b) S —Br -tert-butyl —H F189 (a and b) S —Br -iso-propyl—H F190 (a and b) S —Br —CH₃ —CH₃ F191 (a and b) S —Br —H —H F192 (a andb) S —Br —H —Cl F193 (a and b) S —Br —H —Br F194 (a and b) S —Br —H —FF195 (a and b) S —Br —H —CH₃ F196 (a and b) S —Br —H —CF₃ F197 (a and b)S —Br —H —OCH₃ F198 (a and b) S —Br —H —OCH₂CH₃ F199 (a and b) S —Br —H—OCF₃ F200 (a and b) S —Br —H -tert-butyl F201 (a and b) S —Br —H-iso-propyl F202 (a and b) S —I —Cl —H F203 (a and b) S —I —Br —H F204(a and b) S —I —F —H F205 (a and b) S —I —CH₃ —H F206 (a and b) S —I—CF₃ —H F207 (a and b) S —I —OCH₃ —H F208 (a and b) S —I —OCH₂CH₃ —HF209 (a and b) S —I —OCF₃ —H F210 (a and b) S —I -tert-butyl —H F211 (aand b) S —I -iso-propyl —H F212 (a and b) S —I —CH₃ —CH₃ F213 (a and b)S —I —H —H F214 (a and b) S —I —H —Cl F215 (a and b) S —I —H —Br F216 (aand b) S —I —H —F F217 (a and b) S —I —H —CH₃ F218 (a and b) S —I —H—CF₃ F219 (a and b) S —I —H —OCH₃ F220 (a and b) S —I —H —OCH₂CH₃ F221(a and b) S —I —H —OCF₃ F222 (a and b) S —I —H -tert-butyl F223 (a andb) S —I —H -iso-propyl F224 (a and b) O —H —Cl —H F225 (a and b) O —H—Br —H F226 (a and b) O —H —F —H F227 (a and b) O —H —CH₃ —H F228 (a andb) O —H —CF₃ —H F229 (a and b) O —H —OCH₃ —H F230 (a and b) O —H—OCH₂CH₃ —H F231 (a and b) O —H —OCF₃ —H F232 (a and b) O —H -tert-butyl—H F233 (a and b) O —H -iso-propyl —H F234 (a and b) O —H —CH₃ —CH₃ F235(a and b) O —H —H —H F236 (a and b) O —H —H —Cl F237 (a and b) O —H —H—Br F238 (a and b) O —H —H —F F239 (a and b) O —H —H —CH₃ F240 (a and b)O —H —H —CF₃ F241 (a and b) O —H —H —OCH₃ F242 (a and b) O —H —H—OCH₂CH₃ F243 (a and b) O —H —H —OCF₃ F244 (a and b) O —H —H -tert-butylF245 (a and b) O —H —H -iso-propyl F246 (a and b) O —Cl —Cl —H F247 (aand b) O —Cl —Br —H F248 (a and b) O —Cl —F —H F249 (a and b) O —Cl —CH₃—H F250 (a and b) O —Cl —CF₃ —H F251 (a and b) O —Cl —OCH₃ —H F252 (aand b) O —Cl —OCH₂CH₃ —H F253 (a and b) O —Cl —OCF₃ —H F254 (a and b) O—Cl -tert-butyl —H F255 (a and b) O —Cl -iso-propyl —H F256 (a and b) O—Cl —CH₃ —CH₃ F257 (a and b) O —Cl —H —H F258 (a and b) O —Cl —H —ClF259 (a and b) O —Cl —H —Br F260 (a and b) O —Cl —H —F F261 (a and b) O—Cl —H —CH₃ F262 (a and b) O —CI —H —CF₃ F263 (a and b) O —Cl —H —OCH₃F264 (a and b) O —Cl —H —OCH₂CH₃ F265 (a and b) O —Cl —H —OCF₃ F266 (aand b) O —Cl —H -tert-butyl F267 (a and b) O —Cl —H -iso-propyl F268 (aand b) O —Cl —H —OCF₃ F269 (a and b) O —Cl —H -tert-butyl F270 (a and b)O —Cl —H -iso-propyl F271 (a and b) O —CH₃ —Cl —H F272 (a and b) O —CH₃—Br —H F273 (a and b) O —CH₃ —F —H F274 (a and b) O —CH₃ —CH₃ —H F275 (aand b) O —CH₃ —CF₃ —H F276 (a and b) O —CH₃ —OCH₃ —H F277 (a and b) O—CH₃ —OCH₂CH₃ —H F278 (a and b) O —CH₃ —OCF₃ —H F279 (a and b) O —CH₃-tert-butyl —H F280 (a and b) O —CH₃ -iso-propyl —H F281 (a and b) O—CH₃ —CH₃ —CH₃ F282 (a and b) O —CH₃ —H —H F283 (a and b) O —CH₃ —H —ClF284 (a and b) O —CH₃ —H —Br F285 (a and b) O —CH₃ —H —F F286 (a and b)O —CH₃ —H —CH₃ F287 (a and b) O —CH₃ —H —CF₃ F288 (a and b) O —CH₃ —H—OCH₃ F289 (a and b) O —CH₃ —H —OCH₂CH₃ F290 (a and b) O —CH₃ —H —OCF₃F291 (a and b) O —CH₃ —H -tert-butyl F292 (a and b) O —CH₃ —H-iso-propyl F293 (a and b) O —CF₃ —Cl —H F294 (a and b) O —CF₃ —Br —HF295 (a and b) O —CF₃ —F —H F296 (a and b) O —CF₃ —CH₃ —H F297 (a and b)O —CF₃ —CF₃ —H F298 (a and b) O —CF₃ —OCH₃ —H F299 (a and b) O —CF₃—OCH₂CH₃ —H F300 (a and b) O —CF₃ —OCF₃ —H F301 (a and b) O —CF₃-tert-butyl —H F302 (a and b) O —CF₃ -iso-propyl —H F303 (a and b) O—CF₃ —CH₃ —CH₃ F304 (a and b) O —CF₃ —H —H F305 (a and b) O —CF₃ —H —ClF306 (a and b) O —CF₃ —H —Br F307 (a and b) O —CF₃ —H —F F308 (a and b)O —CF₃ —H —CH₃ F309 (a and b) O —CF₃ —H —CF₃ F310 (a and b) O —CF₃ —H—OCH₃ F311 (a and b) O —CF₃ —H —OCH₂CH₃ F312 (a and b) O —CF₃ —H —OCF₃F313 (a and b) O —CF₃ —H -tert-butyl F314 (a and b) O —CF₃ —H-iso-propyl F315 (a and b) O —CHF₂ —Cl —H F316 (a and b) O —CHF₂ —Br —HF317 (a and b) O —CHF₂ —F —H F318 (a and b) O —CHF₂ —CH₃ —H F319 (a andb) O —CHF₂ —CF₃ —H F320 (a and b) O —CHF₂ —OCH₃ —H F321 (a and b) O—CHF₂ —OCH₂CH₃ —H F322 (a and b) O —CHF₂ —OCF₃ —H F323 (a and b) O —CHF₂-tert-butyl —H F324 (a and b) O —CHF₂ -iso-propyl —H F325 (a and b) O—CHF₂ —CH₃ —CH₃ F326 (a and b) O —CHF₂ —H —H F327 (a and b) O —CHF₂ —H—Cl F328 (a and b) O —CHF₂ —H —Br F329 (a and b) O —CHF₂ —H —F F330 (aand b) O —CHF₂ —H —CH₃ F331 (a and b) O —CHF₂ —H —CF₃ F332 (a and b) O—CHF₂ —H —OCH₃ F333 (a and b) O —CHF₂ —H —OCH₂CH₃ F334 (a and b) O —CHF₂—H —OCF₃ F335 (a and b) O —CHF₂ —H -tert-butyl F336 (a and b) O —CHF₂ —H-iso-propyl F337 (a and b) O —OH —Cl —H F338 (a and b) O —OH —Br —H F339(a and b) O —OH —F —H F340 (a and b) O —OH —CH₃ —H F341 (a and b) O —OH—CF₃ —H F342 (a and b) O —OH —OCH₃ —H F343 (a and b) O —OH —OCH₂CH₃ —HF344 (a and b) O —OH —OCF₃ —H F345 (a and b) O —OH -tert-butyl —H F346(a and b) O —OH -iso-propyl —H F347 (a and b) O —OH —CH₃ —CH₃ F348 (aand b) O —OH —H —H F349 (a and b) O —OH —H —Cl F350 (a and b) O —OH —H—Br F351 (a and b) O —OH —H —F F352 (a and b) O —OH —H —CH₃ F353 (a andb) O —OH —H —CF₃ F354 (a and b) O —OH —H —OCH₃ F355 (a and b) O —OH —H—OCH₂CH₃ F356 (a and b) O —OH —H —OCF₃ F357 (a and b) O —OH —H-tert-butyl F358 (a and b) O —OH —H -iso-propyl F359 (a and b) O —NO₂—Cl —H F360 (a and b) O —NO₂ —Br —H F361 (a and b) O —NO₂ —F —H F362 (aand b) O —NO₂ —CH₃ —H F363 (a and b) O —NO₂ —CF₃ —H F364 (a and b) O—NO₂ —OCH₃ —H F365 (a and b) O —NO₂ —OCH₂CH₃ —H F366 (a and b) O —NO₂—OCF₃ —H F367 (a and b) O —NO₂ -tert-butyl —H F368 (a and b) O —NO₂-iso-propyl —H F369 (a and b) O —NO₂ —CH₃ —CH₃ F370 (a and b) O —NO₂ —H—H F371 (a and b) O —NO₂ —H —Cl F372 (a and b) O —NO₂ —H —Br F373 (a andb) O —NO₂ —H —F F374 (a and b) O —NO₂ —H —CH₃ F375 (a and b) O —NO₂ —H—CF₃ F376 (a and b) O —NO₂ —H —OCH₃ F377 (a and b) O —NO₂ —H —OCH₂CH₃F378 (a and b) O —NO₂ —H —OCF₃ F379 (a and b) O —NO₂ —H -tert-butyl F380(a and b) O —NO₂ —H -iso-propyl F381 (a and b) O —CN —Br —H F382 (a andb) O —CN —Cl —H F383 (a and b) O —CN —F —H F384 (a and b) O —CN —CH₃ —HF385 (a and b) O —CN —CF₃ —H F386 (a and b) O —CN —OCH₃ —H F387 (a andb) O —CN —OCH₂CH₃ —H F388 (a and b) O —CN —OCF₃ —H F389 (a and b) O —CN-tert-butyl —H F390 (a and b) O —CN -iso-propyl —H F391 (a and b) O —CN—CH₃ —CH₃ F392 (a and b) O —CN —H —H F393 (a and b) O —CN —H —Cl F394 (aand b) O —CN —H —Br F395 (a and b) O —CN —H —F F396 (a and b) O —CN —H—CH₃ F397 (a and b) O —CN —H —CF₃ F398 (a and b) O —CN —H —OCH₃ F399 (aand b) O —CN —H —OCH₂CH₃ F400 (a and b) O —CN —H —OCF₃ F401 (a and b) O—CN —H -tert-butyl F402 (a and b) O —CN —H -iso-propyl F403 (a and b) O—Br —Br —H F404 (a and b) O —Br —Cl —H F405 (a and b) O —Br —F —H F406(a and b) O —Br —CH₃ —H F407 (a and b) O —Br —CF₃ —H F408 (a and b) O—Br —OCH₃ —H F409 (a and b) O —Br —OCH₂CH₃ —H F410 (a and b) O —Br —OCF₃—H F411 (a and b) O —Br -tert-butyl —H F412 (a and b) O —Br -iso-propyl—H F413 (a and b) O —Br —CH₃ —CH₃ F414 (a and b) O —Br —H —H F415 (a andb) O —Br —H —Cl F416 (a and b) O —Br —H —Br F417 (a and b) O —Br —H —FF418 (a and b) O —Br —H —CH₃ F419 (a and b) O —Br —H —CF₃ F420 (a and b)O —Br —H —OCH₃ F421 (a and b) O —Br —H —OCH₂CH₃ F422 (a and b) O —Br —H—OCF₃ F423 (a and b) O —Br —H -tert-butyl F424 (a and b) O —Br —H-iso-propyl F425 (a and b) O —I —Cl —H F426 (a and b) O —I —Br —H F427(a and b) O —I —F —H F428 (a and b) O —I —CH₃ —H F429 (a and b) O —I—CF₃ —H F430 (a and b) O —I —OCH₃ —H F431 (a and b) O —I —OCH₂CH₃ —HF432 (a and b) O —I —OCF₃ —H F433 (a and b) O —I -tert-butyl —H F434 (aand b) O —I -iso-propyl —H F435 (a and b) O —I —CH₃ —CH₃ F436 (a and b)O —I —H —H F437 (a and b) O —I —H —Cl F438 (a and b) O —I —H —Br F439 (aand b) O —I —H —F F440 (a and b) O —I —H —CH₃ F441 (a and b) O —I —H—CF₃ F442 (a and b) O —I —H —OCH₃ F443 (a and b) O —I —H —OCH₂CH₃ F444(a and b) O —I —H —OCF₃ F445 (a and b) O —I —H -tert-butyl F446 (a andb) O —I —H -iso-propyl F447 (a and b) NH —H —Cl —H F448 (a and b) NH —H—Br —H F449 (a and b) NH —H —F —H F450 (a and b) NH —H —CH₃ —H F451 (aand b) NH —H —CF₃ —H F452 (a and b) NH —H —OCH₃ —H F453 (a and b) NH —H—OCH₂CH₃ —H F454 (a and b) NH —H —OCF₃ —H F455 (a and b) NH —H-tert-butyl —H F456 (a and b) NH —H -iso-propyl —H F457 (a and b) NH —H—CH₃ —CH₃ F458 (a and b) NH —H —H —H F459 (a and b) NH —H —H —Cl F460 (aand b) NH —H —H —Br F461 (a and b) NH —H —H —F F462 (a and b) NH —H —H—CH₃ F463 (a and b) NH —H —H —CF₃ F464 (a and b) NH —H —H —OCH₃ F465 (aand b) NH —H —H —OCH₂CH₃ F466 (a and b) NH —H —H —OCF₃ F467 (a and b) NH—H —H -tert-butyl F468 (a and b) NH —H —H -iso-propyl F469 (a and b) NH—Cl —Cl —H F470 (a and b) NH —Cl —Br —H F471 (a and b) NH —Cl —F —H F472(a and b) NH —Cl —CH₃ —H F473 (a and b) NH —Cl —CF₃ —H F474 (a and b) NH—Cl —OCH₃ —H F475 (a and b) NH —Cl —OCH₂CH₃ —H F476 (a and b) NH —Cl—OCF₃ —H F477 (a and b) NH —Cl -tert-butyl —H F478 (a and b) NH —Cl-iso-propyl —H F479 (a and b) NH —Cl —CH₃ —CH₃ F480 (a and b) NH —Cl —H—H F481 (a and b) NH —Cl —H —Cl F482 (a and b) NH —Cl —H —Br F483 (a andb) NH —Cl —H —F F484 (a and b) NH —Cl —H —CH₃ F485 (a and b) NH —Cl —H—CF₃ F486 (a and b) NH —Cl —H —OCH₃ F487 (a and b) NH —Cl —H —OCH₂CH₃F488 (a and b) NH —Cl —H —OCF₃ F489 (a and b) NH —Cl —H -tert-butyl F490(a and b) NH —Cl —H -iso-propyl F491 (a and b) NH —Cl —H —OCF₃ F492 (aand b) NH —Cl —H -tert-butyl F493 (a and b) NH —Cl —H -iso-propyl F494(a and b) NH —CH₃ —Cl —H F495 (a and b) NH —CH₃ —Br —H F496 (a and b) NH—CH₃ —F —H F497 (a and b) NH —CH₃ —CH₃ —H F498 (a and b) NH —CH₃ —CF₃ —HF499 (a and b) NH —CH₃ —OCH₃ —H F500 (a and b) NH —CH₃ —OCH₂CH₃ —H F501(a and b) NH —CH₃ —OCF₃ —H F502 (a and b) NH —CH₃ -tert-butyl —H F503 (aand b) NH —CH₃ -iso-propyl —H F504 (a and b) NH —CH₃ —CH₃ —CH₃ F505 (aand b) NH —CH₃ —H —H F506 (a and b) NH —CH₃ —H —Cl F507 (a and b) NH—CH₃ —H —Br F508 (a and b) NH —CH₃ —H —F F509 (a and b) NH —CH₃ —H —CH₃F510 (a and b) NH —CH₃ —H —CF₃ F511 (a and b) NH —CH₃ —H —OCH₃ F512 (aand b) NH —CH₃ —H —OCH₂CH₃ F513 (a and b) NH —CH₃ —H —OCF₃ F514 (a andb) NH —CH₃ —H -tert-butyl F515 (a and b) NH —CH₃ —H -iso-propyl F516 (aand b) NH —CF₃ —Cl —H F517 (a and b) NH —CF₃ —Br —H F518 (a and b) NH—CF₃ —F —H F519 (a and b) NH —CF₃ —CH₃ —H F520 (a and b) NH —CF₃ —CF₃ —HF521 (a and b) NH —CF₃ —OCH₃ —H F522 (a and b) NH —CF₃ —OCH₂CH₃ —H F523(a and b) NH —CF₃ —OCF₃ —H F524 (a and b) NH —CF₃ -tert-butyl —H F525 (aand b) NH —CF₃ -iso-propyl —H F526 (a and b) NH —CF₃ —CH₃ —CH₃ F527 (aand b) NH —CF₃ —H —H F528 (a and b) NH —CF₃ —H —Cl F529 (a and b) NH—CF₃ —H —Br F530 (a and b) NH —CF₃ —H —F F531 (a and b) NH —CF₃ —H —CH₃F532 (a and b) NH —CF₃ —H —CF₃ F533 (a and b) NH —CF₃ —H —OCH₃ F534 (aand b) NH —CF₃ —H —OCH₂CH₃ F535 (a and b) NH —CF₃ —H —OCF₃ F536 (a andb) NH —CF₃ —H -tert-butyl F537 (a and b) NH —CF₃ —H -iso-propyl F538 (aand b) NH —CHF₂ —Cl —H F539 (a and b) NH —CHF₂ —Br —H F540 (a and b) NH—CHF₂ —F —H F541 (a and b) NH —CHF₂ —CH₃ —H F542 (a and b) NH —CHF₂ —CF₃—H F543 (a and b) NH —CHF₂ —OCH₃ —H F544 (a and b) NH —CHF₂ —OCH₂CH₃ —HF545 (a and b) NH —CHF₂ —OCF₃ —H F546 (a and b) NH —CHF₂ -tert-butyl —HF547 (a and b) NH —CHF₂ -iso-propyl —H F548 (a and b) NH —CHF₂ —CH₃ —CH₃F549 (a and b) NH —CHF₂ —H —H F550 (a and b) NH —CHF₂ —H —Cl F551 (a andb) NH —CHF₂ —H —Br F552 (a and b) NH —CHF₂ —H —F F553 (a and b) NH —CHF₂—H —CH₃ F554 (a and b) NH —CHF₂ —H —CF₃ F555 (a and b) NH —CHF₂ —H —OCH₃F556 (a and b) NH —CHF₂ —H —OCH₂CH₃ F557 (a and b) NH —CHF₂ —H —OCF₃F558 (a and b) NH —CHF₂ —H -tert-butyl F559 (a and b) NH —CHF₂ —H-iso-propyl F560 (a and b) NH —OH —Cl —H F561 (a and b) NH —OH —Br —HF562 (a and b) NH —OH —F —H F563 (a and b) NH —OH —CH₃ —H F564 (a and b)NH —OH —CF₃ —H F565 (a and b) NH —OH —OCH₃ —H F566 (a and b) NH —OH—OCH₂CH₃ —H F567 (a and b) NH —OH —OCF₃ —H F568 (a and b) NH —OH-tert-butyl —H F569 (a and b) NH —OH -iso-propyl —H F570 (a and b) NH—OH —CH₃ —CH₃ F571 (a and b) NH —OH —H —H F572 (a and b) NH —OH —H —ClF573 (a and b) NH —OH —H —Br F574 (a and b) NH —OH —H —F F575 (a and b)NH —OH —H —CH₃ F576 (a and b) NH —OH —H —CF₃ F577 (a and b) NH —OH —H—OCH₃ F578 (a and b) NH —OH —H —OCH₂CH₃ F579 (a and b) NH —OH —H —OCF₃F580 (a and b) NH —OH —H -tert-butyl F581 (a and b) NH —OH —H-iso-propyl F582 (a and b) NH —NO₂ —Cl —H F583 (a and b) NH —NO₂ —Br —HF584 (a and b) NH —NO₂ —F —H F585 (a and b) NH —NO₂ —CH₃ —H F586 (a andb) NH —NO₂ —CF₃ —H F587 (a and b) NH —NO₂ —OCH₃ —H F588 (a and b) NH—NO₂ —OCH₂CH₃ —H F589 (a and b) NH —NO₂ —OCF₃ —H F590 (a and b) NH —NO₂-tert-butyl —H F591 (a and b) NH —NO₂ -iso-propyl —H F592 (a and b) NH—NO₂ —CH₃ —CH₃ F593 (a and b) NH —NO₂ —H —H F594 (a and b) NH —NO₂ —H—Cl F595 (a and b) NH —NO₂ —H —Br F596 (a and b) NH —NO₂ —H —F F597 (aand b) NH —NO₂ —H —CH₃ F598 (a and b) NH —NO₂ —H —CF₃ F599 (a and b) NH—NO₂ —H —OCH₃ F600 (a and b) NH —NO₂ —H —OCH₂CH₃ F601 (a and b) NH —NO₂—H —OCF₃ F602 (a and b) NH —NO₂ —H -tert-butyl F603 (a and b) NH —NO₂ —H-iso-propyl F604 (a and b) NH —CN —Br —H F605 (a and b) NH —CN —Cl —HF606 (a and b) NH —CN —F —H F607 (a and b) NH —CN —CH₃ —H F608 (a and b)NH —CN —CF₃ —H F609 (a and b) NH —CN —OCH₃ —H F610 (a and b) NH —CN—OCH₂CH₃ —H F611 (a and b) NH —CN —OCF₃ —H F612 (a and b) NH —CN-tert-butyl —H F613 (a and b) NH —CN -iso-propyl —H F614 (a and b) NH—CN —CH₃ —CH₃ F615 (a and b) NH —CN —H —H F616 (a and b) NH —CN —H —ClF617 (a and b) NH —CN —H —Br F618 (a and b) NH —CN —H —F F619 (a and b)NH —CN —H —CH₃ F620 (a and b) NH —CN —H —CF₃ F621 (a and b) NH —CN —H—OCH₃ F622 (a and b) NH —CN —H —OCH₂CH₃ F623 (a and b) NH —CN —H —OCF₃F624 (a and b) NH —CN —H -tert-butyl F625 (a and b) NH —CN —H-iso-propyl F626 (a and b) NH —Br —Br —H F627 (a and b) NH —Br —Cl —HF628 (a and b) NH —Br —F —H F629 (a and b) NH —Br —CH₃ —H F630 (a and b)NH —Br —CF₃ —H F631 (a and b) NH —Br —OCH₃ —H F632 (a and b) NH —Br—OCH₂CH₃ —H F633 (a and b) NH —Br —OCF₃ —H F634 (a and b) NH —Br-tert-butyl —H F635 (a and b) NH —Br -iso-propyl —H F636 (a and b) NH—Br —CH₃ —CH₃ F637 (a and b) NH —Br —H —H F638 (a and b) NH —Br —H —ClF639 (a and b) NH —Br —H —Br F640 (a and b) NH —Br —H —F F641 (a and b)NH —Br —H —CH₃ F642 (a and b) NH —Br —H —CF₃ F643 (a and b) NH —Br —H—OCH₃ F644 (a and b) NH —Br —H —OCH₂CH₃ F645 (a and b) NH —Br —H —OCF₃F646 (a and b) NH —Br —H -tert-butyl F647 (a and b) NH —Br —H-iso-propyl F648 (a and b) NH —I —Cl —H F649 (a and b) NH —I —Br —H F650(a and b) NH —I —F —H F651 (a and b) NH —I —CH₃ —H F652 (a and b) NH —I—CF₃ —H F653 (a and b) NH —I —OCH₃ —H F654 (a and b) NH —I —OCH₂CH₃ —HF655 (a and b) NH —I —OCF₃ —H F656 (a and b) NH —I -tert-butyl —H F657(a and b) NH —I -iso-propyl —H F658 (a and b) NH —I —CH₃ —CH₃ F659 (aand b) NH —I —H —H F660 (a and b) NH —I —H —Cl F661 (a and b) NH —I —H—Br F662 (a and b) NH —I —H —F F663 (a and b) NH —I —H —CH₃ F664 (a andb) NH —I —H —CF₃ F665 (a and b) NH —I —H —OCH₃ F666 (a and b) NH —I —H—OCH₂CH₃ F667 (a and b) NH —I —H —OCF₃ F668 (a and b) NH —I —H-tert-butyl F669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 7 (Ig)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  G01 (a and b) —H —H  G02 (a and b) —H -tert-butyl  G03 (a and b)—H -iso-butyl  G04 (a and b) —H -sec-butyl  G05 (a and b) —H -iso-propyl G06 (a and b) —H -n-propyl  G07 (a and b) —H -cyclohexyl  G08 (a and b)—H -tert-butoxy  G09 (a and b) —H -isopropoxy  G10 (a and b) —H —CF₃ G11 (a and b) —H —CH₂CF₃  G12 (a and b) —H —OCF₃  G13 (a and b) —H —Cl G14 (a and b) —H —Br  G15 (a and b) —H —I  G16 (a and b) —H -n-butyl G17 (a and b) —H —CH₃  G18 (a and b) —H —SCF₃  G19 (a and b) —H—N(CH₂CH₃)₂  G20 (a and b) —H —OCF₂CHF₂  G21 (a and b) —H —C(OH)(CF₃)₂ G22 (a and b) —H -(1,1-dimethyl-pentyl)  G23 (a and b) —H-(1,1-dimethyl-acetic acid) ethyl ester  G24 (a and b) —H —N-piperidinyl G25 (a and b) —Cl —H  G26 (a and b) —Cl -tert-butyl  G27 (a and b) —Cl-iso-butyl  G28 (a and b) —Cl -sec-butyl  G29 (a and b) —Cl -iso-propyl G30 (a and b) —Cl -n-propyl  G31 (a and b) —Cl -cyclohexyl  G32 (a andb) —Cl -tert-butoxy  G33 (a and b) —Cl -isopropoxy  G34 (a and b) —Cl—CF₃  G35 (a and b) —Cl —CH₂CF₃  G36 (a and b) —Cl —OCF₃  G37 (a and b)—Cl —Cl  G38 (a and b) —Cl —Br  G39 (a and b) —Cl —I  G40 (a and b) —Cl-n-butyl  G41 (a and b) —Cl —CH₃  G42 (a and b) —Cl —SCF₃  G43 (a and b)—Cl —N(CH₂CH₃)₂  G44 (a and b) —Cl —OCF₂CHF₂  G45 (a and b) —Cl—C(OH)(CF₃)₂  G46 (a and b) —Cl -(1,1-dimethyl-pentyl)  G47 (a and b)—Cl -(1,1-dimethyl-acetic acid) ethyl ester  G48 (a and b) —Cl—N-piperidinyl  G49 (a and b) —F —H  G50 (a and b) —F -tert-butyl  G51(a and b) —F -iso-butyl  G52 (a and b) —F -sec-butyl  G53 (a and b) —F-iso-propyl  G54 (a and b) —F -n-propyl  G55 (a and b) —F -cyclohexyl G56 (a and b) —F -tert-butoxy  G57 (a and b) —F -isopropoxy  G58 (a andb) —F —CF₃  G59 (a and b) —F —CH₂CF₃  G60 (a and b) —F —OCF₃  G61 (a andb) —F —Cl  G62 (a and b) —F —Br  G63 (a and b) —F —I  G64 (a and b) —F-n-butyl  G65 (a and b) —F —CH₃  G66 (a and b) —F —SCF₃  G67 (a and b)—F —N(CH₂CH₃)₂  G68 (a and b) —F —OCF₂CHF₂  G69 (a and b) —F—C(OH)(CF₃)₂  G70 (a and b) —F -(1,1-dimethyl-pentyl)  G71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester  G72 (a and b) —F —N-piperidinyl G73 (a and b) —CH₃ —H  G74 (a and b) —CH₃ -iso-butyl  G75 (a and b)—CH₃ -tert-butyl  G76 (a and b) —CH₃ -sec-butyl  G77 (a and b) —CH₃-iso-propyl  G78 (a and b) —CH₃ -n-propyl  G79 (a and b) —CH₃-cyclohexyl  G80 (a and b) —CH₃ -tert-butoxy  G81 (a and b) —CH₃-isopropoxy  G82 (a and b) —CH₃ —CF₃  G83 (a and b) —CH₃ —CH₂CF₃  G84 (aand b) —CH₃ —OCF₃  G85 (a and b) —CH₃ —Cl  G86 (a and b) —CH₃ —Br  G87(a and b) —CH₃ —I  G88 (a and b) —CH₃ -n-butyl  G89 (a and b) —CH₃ —CH₃ G90 (a and b) —CH₃ —SCF₃  G91 (a and b) —CH₃ —N(CH₂CH₃)₂  G92 (a and b)—CH₃ —OCF₂CHF₂  G93 (a and b) —CH₃ —C(OH)(CF₃)₂  G94 (a and b) —CH₃-(1,1-dimethyl-pentyl)  G95 (a and b) —CH₃ -(1,1-dimethyl-acetic acid)ethyl ester  G96 (a and b) —CH₃ —N-piperidinyl  G97 (a and b) —CF₃ —H G98 (a and b) —CF₃ -tert-butyl  G99 (a and b) —CF₃ -iso-butyl G100 (aand b) —CF₃ -sec-butyl G101 (a and b) —CF₃ -iso-propyl G102 (a and b)—CF₃ -n-propyl G103 (a and b) —CF₃ -cyclohexyl G104 (a and b) —CF₃-tert-butoxy G105 (a and b) —CF₃ -isopropoxy G106 (a and b) —CF₃ —CF₃G107 (a and b) —CF₃ —CH₂CF₃ G108 (a and b) —CF₃ —OCF₃ G109 (a and b)—CF₃ —Cl G110 (a and b) —CF₃ —Br G111 (a and b) —CF₃ —I G112 (a and b)—CF₃ -n-butyl G113 (a and b) —CF₃ —CH₃ G114 (a and b) —CF₃ —SCF₃ G115 (aand b) —CF₃ —N(CH₂CH₃)₂ G116 (a and b) —CF₃ —OCF₂CHF₂ G117 (a and b)—CF₃ —C(OH)(CF₃)₂ G118 (a and b) —CF₃ -(1,1-dimethyl-pentyl) G119 (a andb) —CF₃ -(1,1-dimethyl-acetic acid) ethyl ester G120 (a and b) —CF₃—N-piperidinyl G121 (a and b) —CHF₂ -tert-butyl G122 (a and b) —CHF₂ —HG123 (a and b) —CHF₂ -iso-butyl G124 (a and b) —CHF₂ -sec-butyl G125 (aand b) —CHF₂ -iso-propyl G126 (a and b) —CHF₂ -n-propyl G127 (a and b)—CHF₂ -cyclohexyl G128 (a and b) —CHF₂ -tert-butoxy G129 (a and b) —CHF₂-isopropoxy G130 (a and b) —CHF₂ —CF₃ G131 (a and b) —CHF₂ —CH₂CF₃ G132(a and b) —CHF₂ —OCF₃ G133 (a and b) —CHF₂ —Cl G134 (a and b) —CHF₂ —BrG135 (a and b) —CHF₂ —I G136 (a and b) —CHF₂ -n-butyl G137 (a and b)—CHF₂ —CH₃ G138 (a and b) —CHF₂ —SCF₃ G139 (a and b) —CHF₂ —N(CH₂CH₃)₂G140 (a and b) —CHF₂ —OCF₂CHF₂ G141 (a and b) —CHF₂ —C(OH)(CF₃)₂ G142 (aand b) —CHF₂ -(1,1-dimethyl-pentyl) G143 (a and b) —CHF₂-(1,1-dimethyl-acetic acid) ethyl ester G144 (a and b) —CHF₂—N-piperidinyl G145 (a and b) —OH —H G146 (a and b) —OH -tert-butyl G147(a and b) —OH -iso-butyl G148 (a and b) —OH -sec-butyl G149 (a and b)—OH -iso-propyl G150 (a and b) —OH -n-propyl G151 (a and b) —OH-cyclohexyl G152 (a and b) —OH -tert-butoxy G153 (a and b) —OH-isopropoxy G154 (a and b) —OH —CF₃ G155 (a and b) —OH —CH₂CF₃ G156 (aand b) —OH —OCF₃ G157 (a and b) —OH —Cl G158 (a and b) —OH —Br G159 (aand b) —OH —I G160 (a and b) —OH -n-butyl G161 (a and b) —OH —CH₃ G162(a and b) —OH —SCF₃ G163 (a and b) —OH —N(CH₂CH₃)₂ G164 (a and b) —OH—OCF₂CHF₂ G165 (a and b) —OH —C(OH)(CF₃)₂ G166 (a and b) —OH-(1,1-dimethyl-pentyl) G167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester G168 (a and b) —OH —N-piperidinyl G169 (a and b) —NO₂ —HG170 (a and b) —NO₂ -tert-butyl G171 (a and b) —NO₂ -iso-butyl G172 (aand b) —NO₂ -sec-butyl G173 (a and b) —NO₂ -iso-propyl G174 (a and b)—NO₂ -n-propyl G175 (a and b) —NO₂ -cyclohexyl G176 (a and b) —NO₂-tert-butoxy G177 (a and b) —NO₂ -isopropoxy G178 (a and b) —NO₂ —CF₃G179 (a and b) —NO₂ —CH₂CF₃ G180 (a and b) —NO₂ —OCF₃ G181 (a and b)—NO₂ —Cl G182 (a and b) —NO₂ —Br G183 (a and b) —NO₂ —I G184 (a and b)—NO₂ -n-butyl G185 (a and b) —NO₂ —CH₃ G186 (a and b) —NO₂ —SCF₃ G187 (aand b) —NO₂ —N(CH₂CH₃)₂ G188 (a and b) —NO₂ —OCF₂CHF₂ G189 (a and b)—NO₂ —C(OH)(CF₃)₂ G190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) G191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester G192 (a and b) —NO₂—N-piperidinyl G193 (a and b) —CN —H G194 (a and b) —CN -tert-butyl G195(a and b) —CN -iso-butyl G196 (a and b) —CN -sec-butyl G197 (a and b)—CN -iso-propyl G198 (a and b) —CN -n-propyl G199 (a and b) —CN-cyclohexyl G200 (a and b) —CN -tert-butoxy G201 (a and b) —CN-isopropoxy G202 (a and b) —CN —CF₃ G203 (a and b) —CN —CH₂CF₃ G204 (aand b) —CN —OCF₃ G205 (a and b) —CN —Cl G206 (a and b) —CN —Br G207 (aand b) —CN —I G208 (a and b) —CN -n-butyl G209 (a and b) —CN —CH₃ G210(a and b) —CN —SCF₃ G211 (a and b) —CN —N(CH₂CH₃)₂ G212 (a and b) —CN—OCF₂CHF₂ G213 (a and b) —CN —C(OH)(CF₃)₂ G214 (a and b) —CN-(1,1-dimethyl-pentyl) G215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester G216 (a and b) —CN —N-piperidinyl G217 (a and b) —Br —H G218(a and b) —Br -tert-butyl G219 (a and b) —Br -iso-butyl G220 (a and b)—Br -sec-butyl G221 (a and b) —Br -iso-propyl G222 (a and b) —Br-n-propyl G223 (a and b) —Br -cyclohexyl G224 (a and b) —Br -tert-butoxyG225 (a and b) —Br -isopropoxy G226 (a and b) —Br —CF₃ G227 (a and b)—Br —CH₂CF₃ G228 (a and b) —Br —OCF₃ G229 (a and b) —Br —Cl G230 (a andb) —Br —Br G231 (a and b) —Br —I G232 (a and b) —Br -n-butyl G233 (a andb) —Br —CH₃ G234 (a and b) —Br —SCF₃ G235 (a and b) —Br —N(CH₂CH₃)₂ G236(a and b) —Br —OCF₂CHF₂ G237 (a and b) —Br —C(OH)(CF₃)₂ G238 (a and b)—Br -(1,1-dimethyl-pentyl) G239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester G240 (a and b) —Br —N-piperidinyl G241 (a and b) —I-tert-butyl G242 (a and b) —I —H G243 (a and b) —I -iso-butyl G244 (aand b) —I -sec-butyl G245 (a and b) —I -iso-propyl G246 (a and b) —I-n-propyl G247 (a and b) —I -cyclohexyl G248 (a and b) —I -tert-butoxyG249 (a and b) —I -isopropoxy G250 (a and b) —I —CF₃ G251 (a and b) —I—CH₂CF₃ G252 (a and b) —I —OCF₃ G253 (a and b) —I —Cl G254 (a and b) —I—Br G255 (a and b) —I —I G256 (a and b) —I -n-butyl G257 (a and b) —I—CH₃ G258 (a and b) —I —SCF₃ G259 (a and b) —I —N(CH₂CH₃)₂ G260 (a andb) —I —OCF₂CHF₂ G261 (a and b) —I —C(OH)(CF₃)₂ G262 (a and b) —I-(1,1-dimethyl-pentyl) G263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester G264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 8 (Ih)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b)  H01 (a and b) S —H —Cl —H  H02 (a and b) S —H —Br —H H03 (a and b) S —H —F —H  H04 (a and b) S —H —CH₃ —H  H05 (a and b) S—H —CF₃ —H  H06 (a and b) S —H —OCH₃ —H  H07 (a and b) S —H —OCH₂CH₃ —H H08 (a and b) S —H —OCF₃ —H  H09 (a and b) S —H -tert-butyl —H  H10 (aand b) S —H -iso-propyl —H  H11 (a and b) S —H —CH₃ —CH₃  H12 (a and b)S —H —H —H  H13 (a and b) S —H —H —Cl  H14 (a and b) S —H —H —Br  H15 (aand b) S —H —H —F  H16 (a and b) S —H —H —CH₃  H17 (a and b) S —H —H—CF₃  H18 (a and b) S —H —H —OCH₃  H19 (a and b) S —H —H —OCH₂CH₃  H20(a and b) S —H —H —OCF₃  H21 (a and b) S —H —H -tert-butyl  H22 (a andb) S —H —H -iso-propyl  H23 (a and b) S —Cl —Cl —H  H24 (a and b) S —Cl—Br —H  H25 (a and b) S —Cl —F —H  H26 (a and b) S —Cl —CH₃ —H  H27 (aand b) S —Cl —CF₃ —H  H28 (a and b) S —Cl —OCH₃ —H  H29 (a and b) S —Cl—OCH₂CH₃ —H  H30 (a and b) S —Cl —OCF₃ —H  H31 (a and b) S —Cl-tert-butyl —H  H32 (a and b) S —Cl -iso-propyl —H  H33 (a and b) S —Cl—CH₃ —CH₃  H34 (a and b) S —Cl —H —H  H35 (a and b) S —Cl —H —Cl  H36 (aand b) S —Cl —H —Br  H37 (a and b) S —Cl —H —F  H38 (a and b) S —Cl —H—CH₃  H39 (a and b) S —Cl —H —CF₃  H40 (a and b) S —Cl —H —OCH₃  H41 (aand b) S —Cl —H —OCH₂CH₃  H42 (a and b) S —Cl —H —OCF₃  H43 (a and b) S—Cl —H -tert-butyl  H44 (a and b) S —Cl —H -iso-propyl  H45 (a and b) S—Cl —H —OCF₃  H46 (a and b) S —Cl —H -tert-butyl  H47 (a and b) S —Cl —H-iso-propyl  H48 (a and b) S —CH₃ —Cl —H  H49 (a and b) S —CH₃ —Br —H H50 (a and b) S —CH₃ —F —H  H51 (a and b) S —CH₃ —CH₃ —H  H52 (a and b)S —CH₃ —CF₃ —H  H53 (a and b) S —CH₃ —OCH₃ —H  H54 (a and b) S —CH₃—OCH₂CH₃ —H  H55 (a and b) S —CH₃ —OCF₃ —H  H56 (a and b) S —CH₃-tert-butyl —H  H57 (a and b) S —CH₃ -iso-propyl —H  H58 (a and b) S—CH₃ —CH₃ —CH₃  H59 (a and b) S —CH₃ —H —H  H60 (a and b) S —CH₃ —H —Cl H61 (a and b) S —CH₃ —H —Br  H62 (a and b) S —CH₃ —H —F  H63 (a and b)S —CH₃ —H —CH₃  H64 (a and b) S —CH₃ —H —CF₃  H65 (a and b) S —CH₃ —H—OCH₃  H66 (a and b) S —CH₃ —H —OCH₂CH₃  H67 (a and b) S —CH₃ —H —OCF₃ H68 (a and b) S —CH₃ —H -tert-butyl  H69 (a and b) S —CH₃ —H-iso-propyl  H70 (a and b) S —CF₃ —Cl —H  H71 (a and b) S —CF₃ —Br —H H72 (a and b) S —CF₃ —F —H  H73 (a and b) S —CF₃ —CH₃ —H  H74 (a and b)S —CF₃ —CF₃ —H  H75 (a and b) S —CF₃ —OCH₃ —H  H76 (a and b) S —CF₃—OCH₂CH₃ —H  H77 (a and b) S —CF₃ —OCF₃ —H  H78 (a and b) S —CF₃-tert-butyl —H  H79 (a and b) S —CF₃ -iso-propyl —H  H80 (a and b) S—CF₃ —CH₃ —CH₃  H81 (a and b) S —CF₃ —H —H  H82 (a and b) S —CF₃ —H —Cl H83 (a and b) S —CF₃ —H —Br  H84 (a and b) S —CF₃ —H —F  H85 (a and b)S —CF₃ —H —CH₃  H86 (a and b) S —CF₃ —H —CF₃  H87 (a and b) S —CF₃ —H—OCH₃  H88 (a and b) S —CF₃ —H —OCH₂CH₃  H89 (a and b) S —CF₃ —H —OCF₃ H90 (a and b) S —CF₃ —H -tert-butyl  H91 (a and b) S —CF₃ —H-iso-propyl  H92 (a and b) S —CHF₂ —Cl —H  H93 (a and b) S —CHF₂ —Br —H H94 (a and b) S —CHF₂ —F —H  H95 (a and b) S —CHF₂ —CH₃ —H  H96 (a andb) S —CHF₂ —CF₃ —H  H97 (a and b) S —CHF₂ —OCH₃ —H  H98 (a and b) S—CHF₂ —OCH₂CH₃ —H  H99 (a and b) S —CHF₂ —OCF₃ —H H100 (a and b) S —CHF₂-tert-butyl —H H101 (a and b) S —CHF₂ -iso-propyl —H H102 (a and b) S—CHF₂ —CH₃ —CH₃ H103 (a and b) S —CHF₂ —H —H H104 (a and b) S —CHF₂ —H—Cl H105 (a and b) S —CHF₂ —H —Br H106 (a and b) S —CHF₂ —H —F H107 (aand b) S —CHF₂ —H —CH₃ H108 (a and b) S —CHF₂ —H —CF₃ H109 (a and b) S—CHF₂ —H —OCH₃ H110 (a and b) S —CHF₂ —H —OCH₂CH₃ H111 (a and b) S —CHF₂—H —OCF₃ H112 (a and b) S —CHF₂ —H -tert-butyl H113 (a and b) S —CHF₂ —H-iso-propyl H114 (a and b) S —OH —Cl —H H115 (a and b) S —OH —Br —H H116(a and b) S —OH —F —H H117 (a and b) S —OH —CH₃ —H H118 (a and b) S —OH—CF₃ —H H119 (a and b) S —OH —OCH₃ —H H120 (a and b) S —OH —OCH₂CH₃ —HH121 (a and b) S —OH —OCF₃ —H H122 (a and b) S —OH -tert-butyl —H H123(a and b) S —OH -iso-propyl —H H124 (a and b) S —OH —CH₃ —CH₃ H125 (aand b) S —OH —H —H H126 (a and b) S —OH —H —Cl H127 (a and b) S —OH —H—Br H128 (a and b) S —OH —H —F H129 (a and b) S —OH —H —CH₃ H130 (a andb) S —OH —H —CF₃ H131 (a and b) S —OH —H —OCH₃ H132 (a and b) S —OH —H—OCH₂CH₃ H133 (a and b) S —OH —H —OCF₃ H134 (a and b) S —OH —H-tert-butyl H135 (a and b) S —OH —H -iso-propyl H136 (a and b) S —NO₂—Cl —H H137 (a and b) S —NO₂ —Br —H H138 (a and b) S —NO₂ —F —H H139 (aand b) S —NO₂ —CH₃ —H H140 (a and b) S —NO₂ —CF₃ —H H141 (a and b) S—NO₂ —OCH₃ —H H142 (a and b) S —NO₂ —OCH₂CH₃ —H H143 (a and b) S —NO₂—OCF₃ —H H144 (a and b) S —NO₂ -tert-butyl —H H145 (a and b) S —NO₂-iso-propyl —H H146 (a and b) S —NO₂ —CH₃ —CH₃ H147 (a and b) S —NO₂ —H—H H148 (a and b) S —NO₂ —H —Cl H149 (a and b) S —NO₂ —H —Br H150 (a andb) S —NO₂ —H —F H151 (a and b) S —NO₂ —H —CH₃ H152 (a and b) S —NO₂ —H—CF₃ H153 (a and b) S —NO₂ —H —OCH₃ H154 (a and b) S —NO₂ —H —OCH₂CH₃H155 (a and b) S —NO₂ —H —OCF₃ H156 (a and b) S —NO₂ —H -tert-butyl H157(a and b) S —NO₂ —H -iso-propyl H158 (a and b) S —CN —Br —H H159 (a andb) S —CN —Cl —H H160 (a and b) S —CN —F —H H161 (a and b) S —CN —CH₃ —HH162 (a and b) S —CN —CF₃ —H H163 (a and b) S —CN —OCH₃ —H H164 (a andb) S —CN —OCH₂CH₃ —H H165 (a and b) S —CN —OCF₃ —H H166 (a and b) S —CN-tert-butyl —H H167 (a and b) S —CN -iso-propyl —H H168 (a and b) S —CN—CH₃ —CH₃ H169 (a and b) S —CN —H —H H170 (a and b) S —CN —H —Cl H171 (aand b) S —CN —H —Br H172 (a and b) S —CN —H —F H173 (a and b) S —CN —H—CH₃ H174 (a and b) S —CN —H —CF₃ H175 (a and b) S —CN —H —OCH₃ H176 (aand b) S —CN —H —OCH₂CH₃ H177 (a and b) S —CN —H —OCF₃ H178 (a and b) S—CN —H -tert-butyl H179 (a and b) S —CN —H -iso-propyl H180 (a and b) S—Br —Br —H H181 (a and b) S —Br —Cl —H H182 (a and b) S —Br —F —H H183(a and b) S —Br —CH₃ —H H184 (a and b) S —Br —CF₃ —H H185 (a and b) S—Br —OCH₃ —H H186 (a and b) S —Br —OCH₂CH₃ —H H187 (a and b) S —Br —OCF₃—H H188 (a and b) S —Br -tert-butyl —H H189 (a and b) S —Br -iso-propyl—H H190 (a and b) S —Br —CH₃ —CH₃ H191 (a and b) S —Br —H —H H192 (a andb) S —Br —H —Cl H193 (a and b) S —Br —H —Br H194 (a and b) S —Br —H —FH195 (a and b) S —Br —H —CH₃ H196 (a and b) S —Br —H —CF₃ H197 (a and b)S —Br —H —OCH₃ H198 (a and b) S —Br —H —OCH₂CH₃ H199 (a and b) S —Br —H—OCF₃ H200 (a and b) S —Br —H -tert-butyl H201 (a and b) S —Br —H-iso-propyl H202 (a and b) S —I —Cl —H H203 (a and b) S —I —Br —H H204(a and b) S —I —F —H H205 (a and b) S —I —CH₃ —H H206 (a and b) S —I—CF₃ —H H207 (a and b) S —I —OCH₃ —H H208 (a and b) S —I —OCH₂CH₃ —HH209 (a and b) S —I —OCF₃ —H H210 (a and b) S —I -tert-butyl —H H211 (aand b) S —I -iso-propyl —H H212 (a and b) S —I —CH₃ —CH₃ H213 (a and b)S —I —H —H H214 (a and b) S —I —H —Cl H215 (a and b) S —I —H —Br H216 (aand b) S —I —H —F H217 (a and b) S —I —H —CH₃ H218 (a and b) S —I —H—CF₃ H219 (a and b) S —I —H —OCH₃ H220 (a and b) S —I —H —OCH₂CH₃ H221(a and b) S —I —H —OCF₃ H222 (a and b) S —I —H -tert-butyl H223 (a andb) S —I —H -iso-propyl H224 (a and b) O —H —Cl —H H225 (a and b) O —H—Br —H H226 (a and b) O —H —F —H H227 (a and b) O —H —CH₃ —H H228 (a andb) O —H —CF₃ —H H229 (a and b) O —H —OCH₃ —H H230 (a and b) O —H—OCH₂CH₃ —H H231 (a and b) O —H —OCF₃ —H H232 (a and b) O —H -tert-butyl—H H233 (a and b) O —H -iso-propyl —H H234 (a and b) O —H —CH₃ —CH₃ H235(a and b) O —H —H —H H236 (a and b) O —H —H —Cl H237 (a and b) O —H —H—Br H238 (a and b) O —H —H —F H239 (a and b) O —H —H —CH₃ H240 (a and b)O —H —H —CF₃ H241 (a and b) O —H —H —OCH₃ H242 (a and b) O —H —H—OCH₂CH₃ H243 (a and b) O —H —H —OCF₃ H244 (a and b) O —H —H -tert-butylH245 (a and b) O —H —H -iso-propyl H246 (a and b) O —Cl —Cl —H H247 (aand b) O —Cl —Br —H H248 (a and b) O —Cl —F —H H249 (a and b) O —Cl —CH₃—H H250 (a and b) O —Cl —CF₃ —H H251 (a and b) O —Cl —OCH₃ —H H252 (aand b) O —Cl —OCH₂CH₃ —H H253 (a and b) O —Cl —OCF₃ —H H254 (a and b) O—Cl -tert-butyl —H H255 (a and b) O —Cl -iso-propyl —H H256 (a and b) O—Cl —CH₃ —CH₃ H257 (a and b) O —Cl —H —H H258 (a and b) O —Cl —H —ClH259 (a and b) O —Cl —H —Br H260 (a and b) O —Cl —H —F H261 (a and b) O—Cl —H —CH₃ H262 (a and b) O —Cl —H —CF₃ H263 (a and b) O —Cl —H —OCH₃H264 (a and b) O —Cl —H —OCH₂CH₃ H265 (a and b) O —Cl —H —OCF₃ H266 (aand b) O —Cl —H -tert-butyl H267 (a and b) O —Cl —H -iso-propyl H268 (aand b) O —Cl —H —OCF₃ H269 (a and b) O —Cl —H -tert-butyl H270 (a and b)O —Cl —H -iso-propyl H271 (a and b) O —CH₃ —Cl —H H272 (a and b) O —CH₃—Br —H H273 (a and b) O —CH₃ —F —H H274 (a and b) O —CH₃ —CH₃ —H H275 (aand b) O —CH₃ —CF₃ —H H276 (a and b) O —CH₃ —OCH₃ —H H277 (a and b) O—CH₃ —OCH₂CH₃ —H H278 (a and b) O —CH₃ —OCF₃ —H H279 (a and b) O —CH₃-tert-butyl —H H280 (a and b) O —CH₃ -iso-propyl —H H281 (a and b) O—CH₃ —CH₃ —CH₃ H282 (a and b) O —CH₃ —H —H H283 (a and b) O —CH₃ —H —ClH284 (a and b) O —CH₃ —H —Br H285 (a and b) O —CH₃ —H —F H286 (a and b)O —CH₃ —H —CH₃ H287 (a and b) O —CH₃ —H —CF₃ H288 (a and b) O —CH₃ —H—OCH₃ H289 (a and b) O —CH₃ —H —OCH₂CH₃ H290 (a and b) O —CH₃ —H —OCF₃H291 (a and b) O —CH₃ —H -tert-butyl H292 (a and b) O —CH₃ —H-iso-propyl H293 (a and b) O —CF₃ —Cl —H H294 (a and b) O —CF₃ —Br —HH295 (a and b) O —CF₃ —F —H H296 (a and b) O —CF₃ —CH₃ —H H297 (a and b)O —CF₃ —CF₃ —H H298 (a and b) O —CF₃ —OCH₃ —H H299 (a and b) O —CF₃—OCH₂CH₃ —H H300 (a and b) O —CF₃ —OCF₃ —H H301 (a and b) O —CF₃-tert-butyl —H H302 (a and b) O —CF₃ -iso-propyl —H H303 (a and b) O—CF₃ —CH₃ —CH₃ H304 (a and b) O —CF₃ —H —H H305 (a and b) O —CF₃ —H —ClH306 (a and b) O —CF₃ —H —Br H307 (a and b) O —CF₃ —H —F H308 (a and b)O —CF₃ —H —CH₃ H309 (a and b) O —CF₃ —H —CF₃ H310 (a and b) O —CF₃ —H—OCH₃ H311 (a and b) O —CF₃ —H —OCH₂CH₃ H312 (a and b) O —CF₃ —H —OCF₃H313 (a and b) O —CF₃ —H -tert-butyl H314 (a and b) O —CF₃ —H-iso-propyl H315 (a and b) O —CHF₂ —Cl —H H316 (a and b) O —CHF₂ —Br —HH317 (a and b) O —CHF₂ —F —H H318 (a and b) O —CHF₂ —CH₃ —H H319 (a andb) O —CHF₂ —CF₃ —H H320 (a and b) O —CHF₂ —OCH₃ —H H321 (a and b) O—CHF₂ —OCH₂CH₃ —H H322 (a and b) O —CHF₂ —OCF₃ —H H323 (a and b) O —CHF₂-tert-butyl —H H324 (a and b) O —CHF₂ -iso-propyl —H H325 (a and b) O—CHF₂ —CH₃ —CH₃ H326 (a and b) O —CHF₂ —H —H H327 (a and b) O —CHF₂ —H—Cl H328 (a and b) O —CHF₂ —H —Br H329 (a and b) O —CHF₂ —H —F H330 (aand b) O —CHF₂ —H —CH₃ H331 (a and b) O —CHF₂ —H —CF₃ H332 (a and b) O—CHF₂ —H —OCH₃ H333 (a and b) O —CHF₂ —H —OCH₂CH₃ H334 (a and b) O —CHF₂—H —OCF₃ H335 (a and b) O —CHF₂ —H -tert-butyl H336 (a and b) O —CHF₂ —H-iso-propyl H337 (a and b) O —OH —Cl —H H338 (a and b) O —OH —Br —H H339(a and b) O —OH —F —H H340 (a and b) O —OH —CH₃ —H H341 (a and b) O —OH—CF₃ —H H342 (a and b) O —OH —OCH₃ —H H343 (a and b) O —OH —OCH₂CH₃ —HH344 (a and b) O —OH —OCF₃ —H H345 (a and b) O —OH -tert-butyl —H H346(a and b) O —OH -iso-propyl —H H347 (a and b) O —OH —CH₃ —CH₃ H348 (aand b) O —OH —H —H H349 (a and b) O —OH —H —Cl H350 (a and b) O —OH —H—Br H351 (a and b) O —OH —H —F H352 (a and b) O —OH —H —CH₃ H353 (a andb) O —OH —H —CF₃ H354 (a and b) O —OH —H —OCH₃ H355 (a and b) O —OH —H—OCH₂CH₃ H356 (a and b) O —OH —H —OCF₃ H357 (a and b) O —OH —H-tert-butyl H358 (a and b) O —OH —H -iso-propyl H359 (a and b) O —NO₂—Cl —H H360 (a and b) O —NO₂ —Br —H H361 (a and b) O —NO₂ —F —H H362 (aand b) O —NO₂ —CH₃ —H H363 (a and b) O —NO₂ —CF₃ —H H364 (a and b) O—NO₂ —OCH₃ —H H365 (a and b) O —NO₂ —OCH₂CH₃ —H H366 (a and b) O —NO₂—OCF₃ —H H367 (a and b) O —NO₂ -tert-butyl —H H368 (a and b) O —NO₂-iso-propyl —H H369 (a and b) O —NO₂ —CH₃ —CH₃ H370 (a and b) O —NO₂ —H—H H371 (a and b) O —NO₂ —H —Cl H372 (a and b) O —NO₂ —H —Br H373 (a andb) O —NO₂ —H —F H374 (a and b) O —NO₂ —H —CH₃ H375 (a and b) O —NO₂ —H—CF₃ H376 (a and b) O —NO₂ —H —OCH₃ H377 (a and b) O —NO₂ —H —OCH₂CH₃H378 (a and b) O —NO₂ —H —OCF₃ H379 (a and b) O —NO₂ —H -tert-butyl H380(a and b) O —NO₂ —H -iso-propyl H381 (a and b) O —CN —Br —H H382 (a andb) O —CN —Cl —H H383 (a and b) O —CN —F —H H384 (a and b) O —CN —CH₃ —HH385 (a and b) O —CN —CF₃ —H H386 (a and b) O —CN —OCH₃ —H H387 (a andb) O —CN —OCH₂CH₃ —H H388 (a and b) O —CN —OCF₃ —H H389 (a and b) O —CN-tert-butyl —H H390 (a and b) O —CN -iso-propyl —H H391 (a and b) O —CN—CH₃ —CH₃ H392 (a and b) O —CN —H —H H393 (a and b) O —CN —H —Cl H394 (aand b) O —CN —H —Br H395 (a and b) O —CN —H —F H396 (a and b) O —CN —H—CH₃ H397 (a and b) O —CN —H —CF₃ H398 (a and b) O —CN —H —OCH₃ H399 (aand b) O —CN —H —OCH₂CH₃ H400 (a and b) O —CN —H —OCF₃ H401 (a and b) O—CN —H -tert-butyl H402 (a and b) O —CN —H -iso-propyl H403 (a and b) O—Br —Br —H H404 (a and b) O —Br —Cl —H H405 (a and b) O —Br —F —H H406(a and b) O —Br —CH₃ —H H407 (a and b) O —Br —CF₃ —H H408 (a and b) O—Br —OCH₃ —H H409 (a and b) O —Br —OCH₂CH₃ —H H410 (a and b) O —Br —OCF₃—H H411 (a and b) O —Br -tert-butyl —H H412 (a and b) O —Br -iso-propyl—H H413 (a and b) O —Br —CH₃ —CH₃ H414 (a and b) O —Br —H —H H415 (a andb) O —Br —H —Cl H416 (a and b) O —Br —H —Br H417 (a and b) O —Br —H —FH418 (a and b) O —Br —H —CH₃ H419 (a and b) O —Br —H —CF₃ H420 (a and b)O —Br —H —OCH₃ H421 (a and b) O —Br —H —OCH₂CH₃ H422 (a and b) O —Br —H—OCF₃ H423 (a and b) O —Br —H -tert-butyl H424 (a and b) O —Br —H-iso-propyl H425 (a and b) O —I —Cl —H H426 (a and b) O —I —Br —H H427(a and b) O —I —F —H H428 (a and b) O —I —CH₃ —H H429 (a and b) O —I—CF₃ —H H430 (a and b) O —I —OCH₃ —H H431 (a and b) O —I —OCH₂CH₃ —HH432 (a and b) O —I —OCF₃ —H H433 (a and b) O —I -tert-butyl —H H434 (aand b) O —I -iso-propyl —H H435 (a and b) O —I —CH₃ —CH₃ H436 (a and b)O —I —H —H H437 (a and b) O —I —H —Cl H438 (a and b) O —I —H —Br H439 (aand b) O —I —H —F H440 (a and b) O —I —H —CH₃ H441 (a and b) O —I —H—CF₃ H442 (a and b) O —I —H —OCH₃ H443 (a and b) O —I —H —OCH₂CH₃ H444(a and b) O —I —H —OCF₃ H445 (a and b) O —I —H -tert-butyl H446 (a andb) O —I —H -iso-propyl H447 (a and b) NH —H —Cl —H H448 (a and b) NH —H—Br —H H449 (a and b) NH —H —F —H H450 (a and b) NH —H —CH₃ —H H451 (aand b) NH —H —CF₃ —H H452 (a and b) NH —H —OCH₃ —H H453 (a and b) NH —H—OCH₂CH₃ —H H454 (a and b) NH —H —OCF₃ —H H455 (a and b) NH —H-tert-butyl —H H456 (a and b) NH —H -iso-propyl —H H457 (a and b) NH —H—CH₃ —CH₃ H458 (a and b) NH —H —H —H H459 (a and b) NH —H —H —Cl H460 (aand b) NH —H —H —Br H461 (a and b) NH —H —H —F H462 (a and b) NH —H —H—CH₃ H463 (a and b) NH —H —H —CF₃ H464 (a and b) NH —H —H —OCH₃ H465 (aand b) NH —H —H —OCH₂CH₃ H466 (a and b) NH —H —H —OCF₃ H467 (a and b) NH—H —H -tert-butyl H468 (a and b) NH —H —H -iso-propyl H469 (a and b) NH—Cl —Cl —H H470 (a and b) NH —Cl —Br —H H471 (a and b) NH —Cl —F —H H472(a and b) NH —Cl —CH₃ —H H473 (a and b) NH —Cl —CF₃ —H H474 (a and b) NH—Cl —OCH₃ —H H475 (a and b) NH —Cl —OCH₂CH₃ —H H476 (a and b) NH —Cl—OCF₃ —H H477 (a and b) NH —Cl -tert-butyl —H H478 (a and b) NH —Cl-iso-propyl —H H479 (a and b) NH —Cl —CH₃ —CH₃ H480 (a and b) NH —Cl —H—H H481 (a and b) NH —Cl —H —Cl H482 (a and b) NH —Cl —H —Br H483 (a andb) NH —Cl —H —F H484 (a and b) NH —Cl —H —CH₃ H485 (a and b) NH —Cl —H—CF₃ H486 (a and b) NH —Cl —H —OCH₃ H487 (a and b) NH —Cl —H —OCH₂CH₃H488 (a and b) NH —Cl —H —OCF₃ H489 (a and b) NH —Cl —H -tert-butyl H490(a and b) NH —Cl —H -iso-propyl H491 (a and b) NH —Cl —H —OCF₃ H492 (aand b) NH —Cl —H -tert-butyl H493 (a and b) NH —Cl —H -iso-propyl H494(a and b) NH —CH₃ —Cl —H H495 (a and b) NH —CH₃ —Br —H H496 (a and b) NH—CH₃ —F —H H497 (a and b) NH —CH₃ —CH₃ —H H498 (a and b) NH —CH₃ —CF₃ —HH499 (a and b) NH —CH₃ —OCH₃ —H H500 (a and b) NH —CH₃ —OCH₂CH₃ —H H501(a and b) NH —CH₃ —OCF₃ —H H502 (a and b) NH —CH₃ -tert-butyl —H H503 (aand b) NH —CH₃ -iso-propyl —H H504 (a and b) NH —CH₃ —CH₃ —CH₃ H505 (aand b) NH —CH₃ —H —H H506 (a and b) NH —CH₃ —H —Cl H507 (a and b) NH—CH₃ —H —Br H508 (a and b) NH —CH₃ —H —F H509 (a and b) NH —CH₃ —H —CH₃H510 (a and b) NH —CH₃ —H —CF₃ H511 (a and b) NH —CH₃ —H —OCH₃ H512 (aand b) NH —CH₃ —H —OCH₂CH₃ H513 (a and b) NH —CH₃ —H —OCF₃ H514 (a andb) NH —CH₃ —H -tert-butyl H515 (a and b) NH —CH₃ —H -iso-propyl H516 (aand b) NH —CF₃ —Cl —H H517 (a and b) NH —CF₃ —Br —H H518 (a and b) NH—CF₃ —F —H H519 (a and b) NH —CF₃ —CH₃ —H H520 (a and b) NH —CF₃ —CF₃ —HH521 (a and b) NH —CF₃ —OCH₃ —H H522 (a and b) NH —CF₃ —OCH₂CH₃ —H H523(a and b) NH —CF₃ —OCF₃ —H H524 (a and b) NH —CF₃ -tert-butyl —H H525 (aand b) NH —CF₃ -iso-propyl —H H526 (a and b) NH —CF₃ —CH₃ —CH₃ H527 (aand b) NH —CF₃ —H —H H528 (a and b) NH —CF₃ —H —Cl H529 (a and b) NH—CF₃ —H —Br H530 (a and b) NH —CF₃ —H —F H531 (a and b) NH —CF₃ —H —CH₃H532 (a and b) NH —CF₃ —H —CF₃ H533 (a and b) NH —CF₃ —H —OCH₃ H534 (aand b) NH —CF₃ —H —OCH₂CH₃ H535 (a and b) NH —CF₃ —H —OCF₃ H536 (a andb) NH —CF₃ —H -tert-butyl H537 (a and b) NH —CF₃ —H -iso-propyl H538 (aand b) NH —CHF₂ —Cl —H H539 (a and b) NH —CHF₂ —Br —H H540 (a and b) NH—CHF₂ —F —H H541 (a and b) NH —CHF₂ —CH₃ —H H542 (a and b) NH —CHF₂ —CF₃—H H543 (a and b) NH —CHF₂ —OCH₃ —H H544 (a and b) NH —CHF₂ —OCH₂CH₃ —HH545 (a and b) NH —CHF₂ —OCF₃ —H H546 (a and b) NH —CHF₂ -tert-butyl —HH547 (a and b) NH —CHF₂ -iso-propyl —H H548 (a and b) NH —CHF₂ —CH₃ —CH₃H549 (a and b) NH —CHF₂ —H —H H550 (a and b) NH —CHF₂ —H —Cl H551 (a andb) NH —CHF₂ —H —Br H552 (a and b) NH —CHF₂ —H —F H553 (a and b) NH —CHF₂—H —CH₃ H554 (a and b) NH —CHF₂ —H —CF₃ H555 (a and b) NH —CHF₂ —H —OCH₃H556 (a and b) NH —CHF₂ —H —OCH₂CH₃ H557 (a and b) NH —CHF₂ —H —OCF₃H558 (a and b) NH —CHF₂ —H -tert-butyl H559 (a and b) NH —CHF₂ —H-iso-propyl H560 (a and b) NH —OH —Cl —H H561 (a and b) NH —OH —Br —HH562 (a and b) NH —OH —F —H H563 (a and b) NH —OH —CH₃ —H H564 (a and b)NH —OH —CF₃ —H H565 (a and b) NH —OH —OCH₃ —H H566 (a and b) NH —OH—OCH₂CH₃ —H H567 (a and b) NH —OH —OCF₃ —H H568 (a and b) NH —OH-tert-butyl —H H569 (a and b) NH —OH -iso-propyl —H H570 (a and b) NH—OH —CH₃ —CH₃ H571 (a and b) NH —OH —H —H H572 (a and b) NH —OH —H —ClH573 (a and b) NH —OH —H —Br H574 (a and b) NH —OH —H —F H575 (a and b)NH —OH —H —CH₃ H576 (a and b) NH —OH —H —CF₃ H577 (a and b) NH —OH —H—OCH₃ H578 (a and b) NH —OH —H —OCH₂CH₃ H579 (a and b) NH —OH —H —OCF₃H580 (a and b) NH —OH —H -tert-butyl H581 (a and b) NH —OH —H-iso-propyl H582 (a and b) NH —NO₂ —Cl —H H583 (a and b) NH —NO₂ —Br —HH584 (a and b) NH —NO₂ —F —H H585 (a and b) NH —NO₂ —CH₃ —H H586 (a andb) NH —NO₂ —CF₃ —H H587 (a and b) NH —NO₂ —OCH₃ —H H588 (a and b) NH—NO₂ —OCH₂CH₃ —H H589 (a and b) NH —NO₂ —OCF₃ —H H590 (a and b) NH —NO₂-tert-butyl —H H591 (a and b) NH —NO₂ -iso-propyl —H H592 (a and b) NH—NO₂ —CH₃ —CH₃ H593 (a and b) NH —NO₂ —H —H H594 (a and b) NH —NO₂ —H—Cl H595 (a and b) NH —NO₂ —H —Br H596 (a and b) NH —NO₂ —H —F H597 (aand b) NH —NO₂ —H —CH₃ H598 (a and b) NH —NO₂ —H —CF₃ H599 (a and b) NH—NO₂ —H —OCH₃ H600 (a and b) NH —NO₂ —H —OCH₂CH₃ H601 (a and b) NH —NO₂—H —OCF₃ H602 (a and b) NH —NO₂ —H -tert-butyl H603 (a and b) NH —NO₂ —H-iso-propyl H604 (a and b) NH —CN —Br —H H605 (a and b) NH —CN —Cl —HH606 (a and b) NH —CN —F —H H607 (a and b) NH —CN —CH₃ —H H608 (a and b)NH —CN —CF₃ —H H609 (a and b) NH —CN —OCH₃ —H H610 (a and b) NH —CN—OCH₂CH₃ —H H611 (a and b) NH —CN —OCF₃ —H H612 (a and b) NH —CN-tert-butyl —H H613 (a and b) NH —CN -iso-propyl —H H614 (a and b) NH—CN —CH₃ —CH₃ H615 (a and b) NH —CN —H —H H616 (a and b) NH —CN —H —ClH617 (a and b) NH —CN —H —Br H618 (a and b) NH —CN —H —F H619 (a and b)NH —CN —H —CH₃ H620 (a and b) NH —CN —H —CF₃ H621 (a and b) NH —CN —H—OCH₃ H622 (a and b) NH —CN —H —OCH₂CH₃ H623 (a and b) NH —CN —H —OCF₃H624 (a and b) NH —CN —H -tert-butyl H625 (a and b) NH —CN —H-iso-propyl H626 (a and b) NH —Br —Br —H H627 (a and b) NH —Br —Cl —HH628 (a and b) NH —Br —F —H H629 (a and b) NH —Br —CH₃ —H H630 (a and b)NH —Br —CF₃ —H H631 (a and b) NH —Br —OCH₃ —H H632 (a and b) NH —Br—OCH₂CH₃ —H H633 (a and b) NH —Br —OCF₃ —H H634 (a and b) NH —Br-tert-butyl —H H635 (a and b) NH —Br -iso-propyl —H H636 (a and b) NH—Br —CH₃ —CH₃ H637 (a and b) NH —Br —H —H H638 (a and b) NH —Br —H —ClH639 (a and b) NH —Br —H —Br H640 (a and b) NH —Br —H —F H641 (a and b)NH —Br —H —CH₃ H642 (a and b) NH —Br —H —CF₃ H643 (a and b) NH —Br —H—OCH₃ H644 (a and b) NH —Br —H —OCH₂CH₃ H645 (a and b) NH —Br —H —OCF₃H646 (a and b) NH —Br —H -tert-butyl H647 (a and b) NH —Br —H-iso-propyl H648 (a and b) NH —I —Cl —H H649 (a and b) NH —I —Br —H H650(a and b) NH —I —F —H H651 (a and b) NH —I —CH₃ —H H652 (a and b) NH —I—CF₃ —H H653 (a and b) NH —I —OCH₃ —H H654 (a and b) NH —I —OCH₂CH₃ —HH655 (a and b) NH —I —OCF₃ —H H656 (a and b) NH —I -tert-butyl —H H657(a and b) NH —I -iso-propyl —H H658 (a and b) NH —I —CH₃ —CH₃ H659 (aand b) NH —I —H —H H660 (a and b) NH —I —H —Cl H661 (a and b) NH —I —H—Br H662 (a and b) NH —I —H —F H663 (a and b) NH —I —H —CH₃ H664 (a andb) NH —I —H —CF₃ H665 (a and b) NH —I —H —OCH₃ H666 (a and b) NH —I —H—OCH₂CH₃ H667 (a and b) NH —I —H —OCF₃ H668 (a and b) NH —I —H-tert-butyl H669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 9 (Ii)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  I01 (a and b) —H —H  I02 (a and b) —H -tert-butyl  I03 (a and b)—H -iso-butyl  I04 (a and b) —H -sec-butyl  I05 (a and b) —H -iso-propyl I06 (a and b) —H -n-propyl  I07 (a and b) —H -cyclohexyl  I08 (a and b)—H -tert-butoxy  I09 (a and b) —H -isopropoxy  I10 (a and b) —H —CF₃ I11 (a and b) —H —CH₂CF₃  I12 (a and b) —H —OCF₃  I13 (a and b) —H —Cl I14 (a and b) —H —Br  I15 (a and b) —H —I  I16 (a and b) —H -n-butyl I17 (a and b) —H —CH₃  I18 (a and b) —H —SCF₃  I19 (a and b) —H—N(CH₂CH₃)₂  I20 (a and b) —H —OCF₂CHF₂  I21 (a and b) —H —C(OH)(CF₃)₂ I22 (a and b) —H -(1,1-dimethyl-pentyl)  I23 (a and b) —H-(1,1-dimethyl-acetic acid) ethyl ester  I24 (a and b) —H —N-piperidinyl I25 (a and b) —Cl —H  I26 (a and b) —Cl -tert-butyl  I27 (a and b) —Cl-iso-butyl  I28 (a and b) —Cl -sec-butyl  I29 (a and b) —Cl -iso-propyl I30 (a and b) —Cl -n-propyl  I31 (a and b) —Cl -cyclohexyl  I32 (a andb) —Cl -tert-butoxy  I33 (a and b) —Cl -isopropoxy  I34 (a and b) —Cl—CF₃  I35 (a and b) —Cl —CH₂CF₃  I36 (a and b) —Cl —OCF₃  I37 (a and b)—Cl —Cl  I38 (a and b) —Cl —Br  I39 (a and b) —Cl —I  I40 (a and b) —Cl-n-butyl  I41 (a and b) —Cl —CH₃  I42 (a and b) —Cl —SCF₃  I43 (a and b)—Cl —N(CH₂CH₃)₂  I44 (a and b) —Cl —OCF₂CHF₂  I45 (a and b) —Cl—C(OH)(CF₃)₂  I46 (a and b) —Cl -(1,1-dimethyl-pentyl)  I47 (a and b)—Cl -(1,1-dimethyl-acetic acid) ethyl ester  I48 (a and b) —Cl—N-piperidinyl  I49 (a and b) —F —H  I50 (a and b) —F -tert-butyl  I51(a and b) —F -iso-butyl  I52 (a and b) —F -sec-butyl  I53 (a and b) —F-iso-propyl  I54 (a and b) —F -n-propyl  I55 (a and b) —F -cyclohexyl I56 (a and b) —F -tert-butoxy  I57 (a and b) —F -isopropoxy  I58 (a andb) —F —CF₃  I59 (a and b) —F —CH₂CF₃  I60 (a and b) —F —OCF₃  I61 (a andb) —F —Cl  I62 (a and b) —F —Br  I63 (a and b) —F —I  I64 (a and b) —F-n-butyl  I65 (a and b) —F —CH₃  I66 (a and b) —F —SCF₃  I67 (a and b)—F —N(CH₂CH₃)₂  I68 (a and b) —F —OCF₂CHF₂  I69 (a and b) —F—C(OH)(CF₃)₂  I70 (a and b) —F -(1,1-dimethyl-pentyl)  I71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester  I72 (a and b) —F —N-piperidinyl I73 (a and b) —CH₃ —H  I74 (a and b) —CH₃ -iso-butyl  I75 (a and b)—CH₃ -tert-butyl  I76 (a and b) —CH₃ -sec-butyl  I77 (a and b) —CH₃-iso-propyl  I78 (a and b) —CH₃ -n-propyl  I79 (a and b) —CH₃-cyclohexyl  I80 (a and b) —CH₃ -tert-butoxy  I81 (a and b) —CH₃-isopropoxy  I82 (a and b) —CH₃ —CF₃  I83 (a and b) —CH₃ —CH₂CF₃  I84 (aand b) —CH₃ —OCF₃  I85 (a and b) —CH₃ —Cl  I86 (a and b) —CH₃ —Br  I87(a and b) —CH₃ —I  I88 (a and b) —CH₃ -n-butyl  I89 (a and b) —CH₃ —CH₃ I90 (a and b) —CH₃ —SCF₃  I91 (a and b) —CH₃ —N(CH₂CH₃)₂  I92 (a and b)—CH₃ —OCF₂CHF₂  I93 (a and b) —CH₃ —C(OH)(CF₃)₂  I94 (a and b) —CH₃-(1,1-dimethyl-pentyl)  I95 (a and b) —CH₃ -(1,1-dimethyl-acetic acid)ethyl ester  I96 (a and b) —CH₃ —N-piperidinyl  I97 (a and b) —CF₃ —H I98 (a and b) —CF₃ -tert-butyl  I99 (a and b) —CF₃ -iso-butyl I100 (aand b) —CF₃ -sec-butyl I101 (a and b) —CF₃ -iso-propyl I102 (a and b)—CF₃ -n-propyl I103 (a and b) —CF₃ -cyclohexyl I104 (a and b) —CF₃-tert-butoxy I105 (a and b) —CF₃ -isopropoxy I106 (a and b) —CF₃ —CF₃I107 (a and b) —CF₃ —CH₂CF₃ I108 (a and b) —CF₃ —OCF₃ I109 (a and b)—CF₃ —Cl I110 (a and b) —CF₃ —Br I111 (a and b) —CF₃ —I I112 (a and b)—CF₃ -n-butyl I113 (a and b) —CF₃ —CH₃ I114 (a and b) —CF₃ —SCF₃ I115 (aand b) —CF₃ —N(CH₂CH₃)₂ I116 (a and b) —CF₃ —OCF₂CHF₂ I117 (a and b)—CF₃ —C(OH)(CF₃)₂ I118 (a and b) —CF₃ -(1,1-dimethyl-pentyl) I119 (a andb) —CF₃ -(1,1-dimethyl-acetic acid) ethyl ester I120 (a and b) —CF₃—N-piperidinyl I121 (a and b) —CHF₂ -tert-butyl I122 (a and b) —CHF₂ —HI123 (a and b) —CHF₂ -iso-butyl I124 (a and b) —CHF₂ -sec-butyl I125 (aand b) —CHF₂ -iso-propyl I126 (a and b) —CHF₂ -n-propyl I127 (a and b)—CHF₂ -cyclohexyl I128 (a and b) —CHF₂ -tert-butoxy I129 (a and b) —CHF₂-isopropoxy I130 (a and b) —CHF₂ —CF₃ I131 (a and b) —CHF₂ —CH₂CF₃ I132(a and b) —CHF₂ —OCF₃ I133 (a and b) —CHF₂ —Cl I134 (a and b) —CHF₂ —BrI135 (a and b) —CHF₂ —I I136 (a and b) —CHF₂ -n-butyl I137 (a and b)—CHF₂ —CH₃ I138 (a and b) —CHF₂ —SCF₃ I139 (a and b) —CHF₂ —N(CH₂CH₃)₂I140 (a and b) —CHF₂ —OCF₂CHF₂ I141 (a and b) —CHF₂ —C(OH)(CF₃)₂ I142 (aand b) —CHF₂ -(1,1-dimethyl-pentyl) I143 (a and b) —CHF₂-(1,1-dimethyl-acetic acid) ethyl ester I144 (a and b) —CHF₂—N-piperidinyl I145 (a and b) —OH —H I146 (a and b) —OH -tert-butyl I147(a and b) —OH -iso-butyl I148 (a and b) —OH -sec-butyl I149 (a and b)—OH -iso-propyl I150 (a and b) —OH -n-propyl I151 (a and b) —OH-cyclohexyl I152 (a and b) —OH -tert-butoxy I153 (a and b) —OH-isopropoxy I154 (a and b) —OH —CF₃ I155 (a and b) —OH —CH₂CF₃ I156 (aand b) —OH —OCF₃ I157 (a and b) —OH —Cl I158 (a and b) —OH —Br I159 (aand b) —OH —I I160 (a and b) —OH -n-butyl I161 (a and b) —OH —CH₃ I162(a and b) —OH —SCF₃ I163 (a and b) —OH —N(CH₂CH₃)₂ I164 (a and b) —OH—OCF₂CHF₂ I165 (a and b) —OH —C(OH)(CF₃)₂ I166 (a and b) —OH-(1,1-dimethyl-pentyl) I167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester I168 (a and b) —OH —N-piperidinyl I169 (a and b) —NO₂ —HI170 (a and b) —NO₂ -tert-butyl I171 (a and b) —NO₂ -iso-butyl I172 (aand b) —NO₂ -sec-butyl I173 (a and b) —NO₂ -iso-propyl I174 (a and b)—NO₂ -n-propyl I175 (a and b) —NO₂ -cyclohexyl I176 (a and b) —NO₂-tert-butoxy I177 (a and b) —NO₂ -isopropoxy I178 (a and b) —NO₂ —CF₃I179 (a and b) —NO₂ —CH₂CF₃ I180 (a and b) —NO₂ —OCF₃ I181 (a and b)—NO₂ —Cl I182 (a and b) —NO₂ —Br I183 (a and b) —NO₂ —I I184 (a and b)—NO₂ -n-butyl I185 (a and b) —NO₂ —CH₃ I186 (a and b) —NO₂ —SCF₃ I187 (aand b) —NO₂ —N(CH₂CH₃)₂ I188 (a and b) —NO₂ —OCF₂CHF₂ I189 (a and b)—NO₂ —C(OH)(CF₃)₂ I190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) I191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester I192 (a and b) —NO₂—N-piperidinyl I193 (a and b) —CN —H I194 (a and b) —CN -tert-butyl I195(a and b) —CN -iso-butyl I196 (a and b) —CN -sec-butyl I197 (a and b)—CN -iso-propyl I198 (a and b) —CN -n-propyl I199 (a and b) —CN-cyclohexyl I200 (a and b) —CN -tert-butoxy I201 (a and b) —CN-isopropoxy I202 (a and b) —CN —CF₃ I203 (a and b) —CN —CH₂CF₃ I204 (aand b) —CN —OCF₃ I205 (a and b) —CN —Cl I206 (a and b) —CN —Br I207 (aand b) —CN —I I208 (a and b) —CN -n-butyl I209 (a and b) —CN —CH₃ I210(a and b) —CN —SCF₃ I211 (a and b) —CN —N(CH₂CH₃)₂ I212 (a and b) —CN—OCF₂CHF₂ I213 (a and b) —CN —C(OH)(CF₃)₂ I214 (a and b) —CN-(1,1-dimethyl-pentyl) I215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester I216 (a and b) —CN —N-piperidinyl I217 (a and b) —Br —H I218(a and b) —Br -tert-butyl I219 (a and b) —Br -iso-butyl I220 (a and b)—Br -sec-butyl I221 (a and b) —Br -iso-propyl I222 (a and b) —Br-n-propyl I223 (a and b) —Br -cyclohexyl I224 (a and b) —Br -tert-butoxyI225 (a and b) —Br -isopropoxy I226 (a and b) —Br —CF₃ I227 (a and b)—Br —CH₂CF₃ I228 (a and b) —Br —OCF₃ I229 (a and b) —Br —Cl I230 (a andb) —Br —Br I231 (a and b) —Br —I I232 (a and b) —Br -n-butyl I233 (a andb) —Br —CH₃ I234 (a and b) —Br —SCF₃ I235 (a and b) —Br —N(CH₂CH₃)₂ I236(a and b) —Br —OCF₂CHF₂ I237 (a and b) —Br —C(OH)(CF₃)₂ I238 (a and b)—Br -(1,1-dimethyl-pentyl) I239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester I240 (a and b) —Br —N-piperidinyl I241 (a and b) —I-tert-butyl I242 (a and b) —I —H I243 (a and b) —I -iso-butyl I244 (aand b) —I -sec-butyl I245 (a and b) —I -iso-propyl I246 (a and b) —I-n-propyl I247 (a and b) —I -cyclohexyl I248 (a and b) —I -tert-butoxyI249 (a and b) —I -isopropoxy I250 (a and b) —I —CF₃ I251 (a and b) —I—CH₂CF₃ I252 (a and b) —I —OCF₃ I253 (a and b) —I —Cl I254 (a and b) —I—Br I255 (a and b) —I —I I256 (a and b) —I -n-butyl I257 (a and b) —I—CH₃ I258 (a and b) —I —SCF₃ I259 (a and b) —I —N(CH₂CH₃)₂ I260 (a andb) —I —OCF₂CHF₂ I261 (a and b) —I —C(OH)(CF₃)₂ I262 (a and b) —I-(1,1-dimethyl-pentyl) I263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester I264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 10 (Ij)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b)  J1 (a and b) S —H —Cl —H  J2 (a and b) S —H —Br —H J3 (a and b) S —H —F —H  J4 (a and b) S —H —CH₃ —H  J5 (a and b) S —H—CF₃ —H  J6 (a and b) S —H —OCH₃ —H  J7 (a and b) S —H —OCH₂CH₃ —H  J8(a and b) S —H —OCF₃ —H  J9 (a and b) S —H -tert-butyl —H  J10 (a and b)S —H -iso-propyl —H  J11 (a and b) S —H —CH₃ —CH₃  J12 (a and b) S —H —H—H  J13 (a and b) S —H —H —Cl  J14 (a and b) S —H —H —Br  J15 (a and b)S —H —H —F  J16 (a and b) S —H —H —CH₃  J17 (a and b) S —H —H —CF₃  J18(a and b) S —H —H —OCH₃  J19 (a and b) S —H —H —OCH₂CH₃  J20 (a and b) S—H —H —OCF₃  J21 (a and b) S —H —H -tert-butyl  J22 (a and b) S —H —H-iso-propyl  J23 (a and b) S —Cl —Cl —H  J24 (a and b) S —Cl —Br —H  J25(a and b) S —Cl —F —H  J26 (a and b) S —Cl —CH₃ —H  J27 (a and b) S —Cl—CF₃ —H  J28 (a and b) S —Cl —OCH₃ —H  J29 (a and b) S —Cl —OCH₂CH₃ —H J30 (a and b) S —Cl —OCF₃ —H  J31 (a and b) S —Cl -tert-butyl —H  J32(a and b) S —Cl -iso-propyl —H  J33 (a and b) S —Cl —CH₃ —CH₃  J34 (aand b) S —Cl —H —H  J35 (a and b) S —Cl —H —Cl  J36 (a and b) S —Cl —H—Br  J37 (a and b) S —Cl —H —F  J38 (a and b) S —Cl —H —CH₃  J39 (a andb) S —Cl —H —CF₃  J40 (a and b) S —Cl —H —OCH₃  J41 (a and b) S —Cl —H—OCH₂CH₃  J42 (a and b) S —Cl —H —OCF₃  J43 (a and b) S —Cl —H-tert-butyl  J44 (a and b) S —Cl —H -iso-propyl  J45 (a and b) S —Cl —H—OCF₃  J46 (a and b) S —Cl —H -tert-butyl  J47 (a and b) S —Cl —H-iso-propyl  J48 (a and b) S —CH₃ —Cl —H  J49 (a and b) S —CH₃ —Br —H J50 (a and b) S —CH₃ —F —H  J51 (a and b) S —CH₃ —CH₃ —H  J52 (a and b)S —CH₃ —CF₃ —H  J53 (a and b) S —CH₃ —OCH₃ —H  J54 (a and b) S —CH₃—OCH₂CH₃ —H  J55 (a and b) S —CH₃ —OCF₃ —H  J56 (a and b) S —CH₃-tert-butyl —H  J57 (a and b) S —CH₃ -iso-propyl —H  J58 (a and b) S—CH₃ —CH₃ —CH₃  J59 (a and b) S —CH₃ —H —H  J60 (a and b) S —CH₃ —H —Cl J61 (a and b) S —CH₃ —H —Br  J62 (a and b) S —CH₃ —H —F  J63 (a and b)S —CH₃ —H —CH₃  J64 (a and b) S —CH₃ —H —CF₃  J65 (a and b) S —CH₃ —H—OCH₃  J66 (a and b) S —CH₃ —H —OCH₂CH₃  J67 (a and b) S —CH₃ —H —OCF₃ J68 (a and b) S —CH₃ —H -tert-butyl  J69 (a and b) S —CH₃ —H-iso-propyl  J70 (a and b) S —CF₃ —Cl —H  J71 (a and b) S —CF₃ —Br —H J72 (a and b) S —CF₃ —F —H  J73 (a and b) S —CF₃ —CH₃ —H  J74 (a and b)S —CF₃ —CF₃ —H  J75 (a and b) S —CF₃ —OCH₃ —H  J76 (a and b) S —CF₃—OCH₂CH₃ —H  J77 (a and b) S —CF₃ —OCF₃ —H  J78 (a and b) S —CF₃-tert-butyl —H  J79 (a and b) S —CF₃ -iso-propyl —H  J80 (a and b) S—CF₃ —CH₃ —CH₃  J81 (a and b) S —CF₃ —H —H  J82 (a and b) S —CF₃ —H —Cl J83 (a and b) S —CF₃ —H —Br  J84 (a and b) S —CF₃ —H —F  J85 (a and b)S —CF₃ —H —CH₃  J86 (a and b) S —CF₃ —H —CF₃  J87 (a and b) S —CF₃ —H—OCH₃  J88 (a and b) S —CF₃ —H —OCH₂CH₃  J89 (a and b) S —CF₃ —H —OCF₃ J90 (a and b) S —CF₃ —H -cert-butyl  J91 (a and b) S —CF₃ —H-iso-propyl  J92 (a and b) S —CHF₂ —Cl —H  J93 (a and b) S —CHF₂ —Br —H J94 (a and b) S —CHF₂ —F —H  J95 (a and b) S —CHF₂ —CH₃ —H  J96 (a andb) S —CHF₂ —CF₃ —H  J97 (a and b) S —CHF₂ —OCH₃ —H  J98 (a and b) S—CHF₂ —OCH₂CH₃ —H  J99 (a and b) S —CHF₂ —OCF₃ —H J100 (a and b) S —CHF₂-tert-butyl —H J101 (a and b) S —CHF₂ -iso-propyl —H J102 (a and b) S—CHF₂ —CH₃ —CH₃ J103 (a and b) S —CHF₂ —H —H J104 (a and b) S —CHF₂ —H—Cl J105 (a and b) S —CHF₂ —H —Br J106 (a and b) S —CHF₂ —H —F J107 (aand b) S —CHF₂ —H —CH₃ J108 (a and b) S —CHF₂ —H —CF₃ J109 (a and b) S—CHF₂ —H —OCH₃ J110 (a and b) S —CHF₂ —H —OCH₂CH₃ J111 (a and b) S —CHF₂—H —OCF₃ J112 (a and b) S —CHF₂ —H -tert-butyl J113 (a and b) S —CHF₂ —H-iso-propyl J114 (a and b) S —OH —Cl —H J115 (a and b) S —OH —Br —H J116(a and b) S —OH —F —H J117 (a and b) S —OH —CH₃ —H J118 (a and b) S —OH—CF₃ —H J119 (a and b) S —OH —OCH₃ —H J120 (a and b) S —OH —OCH₂CH₃ —HJ121 (a and b) S —OH —OCF₃ —H J122 (a and b) S —OH -tert-butyl —H J123(a and b) S —OH -iso-propyl —H J124 (a and b) S —OH —CH₃ —CH₃ J125 (aand b) S —OH —H —H J126 (a and b) S —OH —H —Cl J127 (a and b) S —OH —H—Br J128 (a and b) S —OH —H —F J129 (a and b) S —OH —H —CH₃ J130 (a andb) S —OH —H —CF₃ J131 (a and b) S —OH —H —OCH₃ J132 (a and b) S —OH —H—OCH₂CH₃ J133 (a and b) S —OH —H —OCF₃ J134 (a and b) S —OH —H-tert-butyl J135 (a and b) S —OH —H -iso-propyl J136 (a and b) S —NO₂—Cl —H J137 (a and b) S —NO₂ —Br —H J138 (a and b) S —NO₂ —F —H J139 (aand b) S —NO₂ —CH₃ —H J140 (a and b) S —NO₂ —CF₃ —H J141 (a and b) S—NO₂ —OCH₃ —H J142 (a and b) S —NO₂ —OCH₂CH₃ —H J143 (a and b) S —NO₂—OCF₃ —H J144 (a and b) S —NO₂ -tert-butyl —H J145 (a and b) S —NO₂-iso-propyl —H J146 (a and b) S —NO₂ —CH₃ —CH₃ J147 (a and b) S —NO₂ —H—H J148 (a and b) S —NO₂ —H —Cl J149 (a and b) S —NO₂ —H —Br J150 (a andb) S —NO₂ —H —F J151 (a and b) S —NO₂ —H —CH₃ J152 (a and b) S —NO₂ —H—CF₃ J153 (a and b) S —NO₂ —H —OCH₃ J154 (a and b) S —NO₂ —H —OCH₂CH₃J155 (a and b) S —NO₂ —H —OCF₃ J156 (a and b) S —NO₂ —H -tert-butyl J157(a and b) S —NO₂ —H -iso-propyl J158 (a and b) S —CN —Br —H J159 (a andb) S —CN —Cl —H J160 (a and b) S —CN —F —H J161 (a and b) S —CN —CH₃ —HJ162 (a and b) S —CN —CF₃ —H J163 (a and b) S —CN —OCH₃ —H J164 (a andb) S —CN —OCH₂CH₃ —H J165 (a and b) S —CN —OCF₃ —H J166 (a and b) S —CN-tert-butyl —H J167 (a and b) S —CN -iso-propyl —H J168 (a and b) S —CN—CH₃ —CH₃ J169 (a and b) S —CN —H —H J170 (a and b) S —CN —H —Cl J171 (aand b) S —CN —H —Br J172 (a and b) S —CN —H —F J173 (a and b) S —CN —H—CH₃ J174 (a and b) S —CN —H —CF₃ J175 (a and b) S —CN —H —OCH₃ J176 (aand b) S —CN —H —OCH₂CH₃ J177 (a and b) S —CN —H —OCF₃ J178 (a and b) S—CN —H -tert-butyl J179 (a and b) S —CN —H -iso-propyl J180 (a and b) S—Br —Br —H J181 (a and b) S —Br —Cl —H J182 (a and b) S —Br —F —H J183(a and b) S —Br —CH₃ —H J184 (a and b) S —Br —CF₃ —H J185 (a and b) S—Br —OCH₃ —H J186 (a and b) S —Br —OCH₂CH₃ —H J187 (a and b) S —Br —OCF₃—H J188 (a and b) S —Br -tert-butyl —H J189 (a and b) S —Br -iso-propyl—H J190 (a and b) S —Br —CH₃ —CH₃ J191 (a and b) S —Br —H —H J192 (a andb) S —Br —H —Cl J193 (a and b) S —Br —H —Br J194 (a and b) S —Br —H —FJ195 (a and b) S —Br —H —CH₃ J196 (a and b) S —Br —H —CF₃ J197 (a and b)S —Br —H —OCH₃ J198 (a and b) S —Br —H —OCH₂CH₃ J199 (a and b) S —Br —H—OCF₃ J200 (a and b) S —Br —H -tert-butyl J201 (a and b) S —Br —H-iso-propyl J202 (a and b) S —I —Cl —H J203 (a and b) S —I —Br —H J204(a and b) S —I —F —H J205 (a and b) S —I —CH₃ —H J206 (a and b) S —I—CF₃ —H J207 (a and b) S —I —OCH₃ —H J208 (a and b) S —I —OCH₂CH₃ —HJ209 (a and b) S —I —OCF₃ —H J210 (a and b) S —I -tert-butyl —H J211 (aand b) S —I -iso-propyl —H J212 (a and b) S —I —CH₃ —CH₃ J213 (a and b)S —I —H —H J214 (a and b) S —I —H —Cl J215 (a and b) S —I —H —Br J216 (aand b) S —I —H —F J217 (a and b) S —I —H —CH₃ J218 (a and b) S —I —H—CF₃ J219 (a and b) S —I —H —OCH₃ J220 (a and b) S —I —H —OCH₂CH₃ J221(a and b) S —I —H —OCF₃ J222 (a and b) S —I —H -tert-butyl J223 (a andb) S —I —H -iso-propyl J224 (a and b) O —H —Cl —H J225 (a and b) O —H—Br —H J226 (a and b) O —H —F —H J227 (a and b) O —H —CH₃ —H J228 (a andb) O —H —CF₃ —H J229 (a and b) O —H —OCH₃ —H J230 (a and b) O —H—OCH₂CH₃ —H J231 (a and b) O —H —OCF₃ —H J232 (a and b) O —H -tert-butyl—H J233 (a and b) O —H -iso-propyl —H J234 (a and b) O —H —CH₃ —CH₃ J235(a and b) O —H —H —H J236 (a and b) O —H —H —Cl J237 (a and b) O —H —H—Br J238 (a and b) O —H —H —F J239 (a and b) O —H —H —CH₃ J240 (a and b)O —H —H —CF₃ J241 (a and b) O —H —H —OCH₃ J242 (a and b) O —H —H—OCH₂CH₃ J243 (a and b) O —H —H —OCF₃ J244 (a and b) O —H —H -tert-butylJ245 (a and b) O —H —H -iso-propyl J246 (a and b) O —Cl —Cl —H J247 (aand b) O —Cl —Br —H J248 (a and b) O —Cl —F —H J249 (a and b) O —Cl —CH₃—H J250 (a and b) O —Cl —CF₃ —H J251 (a and b) O —Cl —OCH₃ —H J252 (aand b) O —Cl —OCH₂CH₃ —H J253 (a and b) O —Cl —OCF₃ —H J254 (a and b) O—Cl -tert-butyl —H J255 (a and b) O —Cl -iso-propyl —H J256 (a and b) O—Cl —CH₃ —CH₃ J257 (a and b) O —Cl —H —H J258 (a and b) O —Cl —H —ClJ259 (a and b) O —Cl —H —Br J260 (a and b) O —Cl —H —F J261 (a and b) O—Cl —H —CH₃ J262 (a and b) O —Cl —H —CF₃ J263 (a and b) O —Cl —H —OCH₃J264 (a and b) O —Cl —H —OCH₂CH₃ J265 (a and b) O —Cl —H —OCF₃ J266 (aand b) O —Cl —H -tert-butyl J267 (a and b) O —Cl —H -iso-propyl J268 (aand b) O —Cl —H —OCF₃ J269 (a and b) O —Cl —H -tert-butyl J270 (a and b)O —Cl —H -iso-propyl J271 (a and b) O —CH₃ —Cl —H J272 (a and b) O —CH₃—Br —H J273 (a and b) O —CH₃ —F —H J274 (a and b) O —CH₃ —CH₃ —H J275 (aand b) O —CH₃ —CF₃ —H J276 (a and b) O —CH₃ —OCH₃ —H J277 (a and b) O—CH₃ —OCH₂CH₃ —H J278 (a and b) O —CH₃ —OCF₃ —H J279 (a and b) O —CH₃-tert-butyl —H J280 (a and b) O —CH₃ -iso-propyl —H J281 (a and b) O—CH₃ —CH₃ —CH₃ J282 (a and b) O —CH₃ —H —H J283 (a and b) O —CH₃ —H —ClJ284 (a and b) O —CH₃ —H —Br J285 (a and b) O —CH₃ —H —F J286 (a and b)O —CH₃ —H —CH₃ J287 (a and b) O —CH₃ —H —CF₃ J288 (a and b) O —CH₃ —H—OCH₃ J289 (a and b) O —CH₃ —H —OCH₂CH₃ J290 (a and b) O —CH₃ —H —OCF₃J291 (a and b) O —CH₃ —H -tert-butyl J292 (a and b) O —CH₃ —H-iso-propyl J293 (a and b) O —CF₃ —Cl —H J294 (a and b) O —CF₃ —Br —HJ295 (a and b) O —CF₃ —F —H J296 (a and b) O —CF₃ —CH₃ —H J297 (a and b)O —CF₃ —CF₃ —H J298 (a and b) O —CF₃ —OCH₃ —H J299 (a and b) O —CF₃—OCH₂CH₃ —H J300 (a and b) O —CF₃ —OCF₃ —H J301 (a and b) O —CF₃-tert-butyl —H J302 (a and b) O —CF₃ -iso-propyl —H J303 (a and b) O—CF₃ —CH₃ —CH₃ J304 (a and b) O —CF₃ —H —H J305 (a and b) O —CF₃ —H —ClJ306 (a and b) O —CF₃ —H —Br J307 (a and b) O —CF₃ —H —F J308 (a and b)O —CF₃ —H —CH₃ J309 (a and b) O —CF₃ —H —CF₃ J310 (a and b) O —CF₃ —H—OCH₃ J311 (a and b) O —CF₃ —H —OCH₂CH₃ J312 (a and b) O —CF₃ —H —OCF₃J313 (a and b) O —CF₃ —H -tert-butyl J314 (a and b) O —CF₃ —H-iso-propyl J315 (a and b) O —CHF₂ —Cl —H J316 (a and b) O —CHF₂ —Br —HJ317 (a and b) O —CHF₂ —F —H J318 (a and b) O —CHF₂ —CH₃ —H J319 (a andb) O —CHF₂ —CF₃ —H J320 (a and b) O —CHF₂ —OCH₃ —H J321 (a and b) O—CHF₂ —OCH₂CH₃ —H J322 (a and b) O —CHF₂ —OCF₃ —H J323 (a and b) O —CHF₂-tert-butyl —H J324 (a and b) O —CHF₂ -iso-propyl —H J325 (a and b) O—CHF₂ —CH₃ —CH₃ J326 (a and b) O —CHF₂ —H —H J327 (a and b) O —CHF₂ —H—Cl J328 (a and b) O —CHF₂ —H —Br J329 (a and b) O —CHF₂ —H —F J330 (aand b) O —CHF₂ —H —CH₃ J331 (a and b) O —CHF₂ —H —CF₃ J332 (a and b) O—CHF₂ —H —OCH₃ J333 (a and b) O —CHF₂ —H —OCH₂CH₃ J334 (a and b) O —CHF₂—H —OCF₃ J335 (a and b) O —CHF₂ —H -tert-butyl J336 (a and b) O —CHF₂ —H-iso-propyl J337 (a and b) O —OH —Cl —H J338 (a and b) O —OH —Br —H J339(a and b) O —OH —F —H J340 (a and b) O —OH —CH₃ —H J341 (a and b) O —OH—CF₃ —H J342 (a and b) O —OH —OCH₃ —H J343 (a and b) O —OH —OCH₂CH₃ —HJ344 (a and b) O —OH —OCF₃ —H J345 (a and b) O —OH -tert-butyl —H J346(a and b) O —OH -iso-propyl —H J347 (a and b) O —OH —CH₃ —CH₃ J348 (aand b) O —OH —H —H J349 (a and b) O —OH —H —Cl J350 (a and b) O —OH —H—Br J351 (a and b) O —OH —H —F J352 (a and b) O —OH —H —CH₃ J353 (a andb) O —OH —H —CF₃ J354 (a and b) O —OH —H —OCH₃ J355 (a and b) O —OH —H—OCH₂CH₃ J356 (a and b) O —OH —H —OCF₃ J357 (a and b) O —OH —H-tert-butyl J358 (a and b) O —OH —H -iso-propyl J359 (a and b) O —NO₂—Cl —H J360 (a and b) O —NO₂ —Br —H J361 (a and b) O —NO₂ —F —H J362 (aand b) O —NO₂ —CH₃ —H J363 (a and b) O —NO₂ —CF₃ —H J364 (a and b) O—NO₂ —OCH₃ —H J365 (a and b) O —NO₂ —OCH₂CH₃ —H J366 (a and b) O —NO₂—OCF₃ —H J367 (a and b) O —NO₂ -tert-butyl —H J368 (a and b) O —NO₂-iso-propyl —H J369 (a and b) O —NO₂ —CH₃ —CH₃ J370 (a and b) O —NO₂ —H—H J371 (a and b) O —NO₂ —H —Cl J372 (a and b) O —NO₂ —H —Br J373 (a andb) O —NO₂ —H —F J374 (a and b) O —NO₂ —H —CH₃ J375 (a and b) O —NO₂ —H—CF₃ J376 (a and b) O —NO₂ —H —OCH₃ J377 (a and b) O —NO₂ —H —OCH₂CH₃J378 (a and b) O —NO₂ —H —OCF₃ J379 (a and b) O —NO₂ —H -tert-butyl J380(a and b) O —NO₂ —H -iso-propyl J381 (a and b) O —CN —Br —H J382 (a andb) O —CN —Cl —H J383 (a and b) O —CN —F —H J384 (a and b) O —CN —CH₃ —HJ385 (a and b) O —CN —CF₃ —H J386 (a and b) O —CN —OCH₃ —H J387 (a andb) O —CN —OCH₂CH₃ —H J388 (a and b) O —CN —OCF₃ —H J389 (a and b) O —CN-tert-butyl —H J390 (a and b) O —CN -iso-propyl —H 3391 (a and b) O —CN—CH₃ —CH₃ J392 (a and b) O —CN —H —H J393 (a and b) O —CN —H —Cl J394 (aand b) O —CN —H —Br J395 (a and b) O —CN —H —F J396 (a and b) O —CN —H—CH₃ J397 (a and b) O —CN —H —CF₃ J398 (a and b) O —CN —H —OCH₃ J399 (aand b) O —CN —H —OCH₂CH₃ 3400 (a and b) O —CN —H —OCF₃ J401 (a and b) O—CN —H -tert-butyl J402 (a and b) O —CN —H -iso-propyl 3403 (a and b) O—Br —Br —H J404 (a and b) O —Br —Cl —H J405 (a and b) O —Br —F —H J406(a and b) O —Br —CH₃ —H J407 (a and b) O —Br —CF₃ —H 3408 (a and b) O—Br —OCH₃ —H J409 (a and b) O —Br —OCH₂CH₃ —H J410 (a and b) O —Br —OCF₃—H 3411 (a and b) O —Br -tert-butyl —H J412 (a and b) O —Br -iso-propyl—H J413 (a and b) O —Br —CH₃ —CH₃ J414 (a and b) O —Br —H —H 3415 (a andb) O —Br —H —Cl J416 (a and b) O —Br —H —Br J417 (a and b) O —Br —H —FJ418 (a and b) O —Br —H —CH₃ J419 (a and b) O —Br —H —CF₃ J420 (a and b)O —Br —H —OCH₃ J421 (a and b) O —Br —H —OCH₂CH₃ J422 (a and b) O —Br —H—OCF₃ J423 (a and b) O —Br —H -tert-butyl J424 (a and b) O —Br —H-iso-propyl J425 (a and b) O —I —Cl —H J426 (a and b) O —I —Br —H J427(a and b) O —I —F —H J428 (a and b) O —I —CH₃ —H J429 (a and b) O —I—CF₃ —H J430 (a and b) O —I —OCH₃ —H J431 (a and b) O —I —OCH₂CH₃ —HJ432 (a and b) O —I —OCF₃ —H J433 (a and b) O —I -tert-butyl —H J434 (aand b) O —I -iso-propyl —H J435 (a and b) O —I —CH₃ —CH₃ J436 (a and b)O —I —H —H J437 (a and b) O —I —H —Cl J438 (a and b) O —I —H —Br J439 (aand b) O —I —H —F J440 (a and b) O —I —H —CH₃ J441 (a and b) O —I —H—CF₃ J442 (a and b) O —I —H —OCH₃ J443 (a and b) O —I —H —OCH₂CH₃ J444(a and b) O —I —H —OCF₃ J445 (a and b) O —I —H -tert-butyl J446 (a andb) O —I —H -iso-propyl J447 (a and b) NH —H —Cl —H J448 (a and b) NH —H—Br —H J449 (a and b) NH —H —F —H J450 (a and b) NH —H —CH₃ —H J451 (aand b) NH —H —CF₃ —H J452 (a and b) NH —H —OCH₃ —H J453 (a and b) NH —H—OCH₂CH₃ —H J454 (a and b) NH —H —OCF₃ —H J455 (a and b) NH —H-tert-butyl —H J456 (a and b) NH —H -iso-propyl —H J457 (a and b) NH —H—CH₃ —CH₃ J458 (a and b) NH —H —H —H J459 (a and b) NH —H —H —Cl J460 (aand b) NH —H —H —Br J461 (a and b) NH —H —H —F J462 (a and b) NH —H —H—CH₃ J463 (a and b) NH —H —H —CF₃ J464 (a and b) NH —H —H —OCH₃ J465 (aand b) NH —H —H —OCH₂CH₃ J466 (a and b) NH —H —H —OCF₃ J467 (a and b) NH—H —H -tert-butyl J468 (a and b) NH —H —H -iso-propyl J469 (a and b) NH—Cl —Cl —H J470 (a and b) NH —Cl —Br —H J471 (a and b) NH —Cl —F —H J472(a and b) NH —Cl —CH₃ —H J473 (a and b) NH —Cl —CF₃ —H J474 (a and b) NH—Cl —OCH₃ —H J475 (a and b) NH —Cl —OCH₂CH₃ —H J476 (a and b) NH —Cl—OCF₃ —H J477 (a and b) NH —Cl -tert-butyl —H J478 (a and b) NH —Cl-iso-propyl —H J479 (a and b) NH —Cl —CH₃ —CH₃ J480 (a and b) NH —Cl —H—H J481 (a and b) NH —Cl —H —Cl J482 (a and b) NH —Cl —H —Br J483 (a andb) NH —Cl —H —F J484 (a and b) NH —Cl —H —CH₃ J485 (a and b) NH —Cl —H—CF₃ J486 (a and b) NH —Cl —H —OCH₃ J487 (a and b) NH —Cl —H —OCH₂CH₃J488 (a and b) NH —Cl —H —OCF₃ J489 (a and b) NH —Cl —H -tert-butyl J490(a and b) NH —Cl —H -iso-propyl J491 (a and b) NH —Cl —H —OCF₃ J492 (aand b) NH —Cl —H -tert-butyl J493 (a and b) NH —Cl —H -iso-propyl J494(a and b) NH —CH₃ —Cl —H J495 (a and b) NH —CH₃ —Br —H J496 (a and b) NH—CH₃ —F —H J497 (a and b) NH —CH₃ —CH₃ —H J498 (a and b) NH —CH₃ —CF₃ —HJ499 (a and b) NH —CH₃ —OCH₃ —H J500 (a and b) NH —CH₃ —OCH₂CH₃ —H J501(a and b) NH —CH₃ —OCF₃ —H J502 (a and b) NH —CH₃ -tert-butyl —H J503 (aand b) NH —CH₃ -iso-propyl —H J504 (a and b) NH —CH₃ —CH₃ —CH₃ J505 (aand b) NH —CH₃ —H —H J506 (a and b) NH —CH₃ —H —Cl J507 (a and b) NH—CH₃ —H —Br J508 (a and b) NH —CH₃ —H —F J509 (a and b) NH —CH₃ —H —CH₃J510 (a and b) NH —CH₃ —H —CF₃ J511 (a and b) NH —CH₃ —H —OCH₃ J512 (aand b) NH —CH₃ —H —OCH₂CH₃ J513 (a and b) NH —CH₃ —H —OCF₃ J514 (a andb) NH —CH₃ —H -tert-butyl J515 (a and b) NH —CH₃ —H -iso-propyl J516 (aand b) NH —CF₃ —Cl —H J517 (a and b) NH —CF₃ —Br —H J518 (a and b) NH—CF₃ —F —H J519 (a and b) NH —CF₃ —CH₃ —H J520 (a and b) NH —CF₃ —CF₃ —HJ521 (a and b) NH —CF₃ —OCH₃ —H J522 (a and b) NH —CF₃ —OCH₂CH₃ —H J523(a and b) NH —CF₃ —OCF₃ —H J524 (a and b) NH —CF₃ -tert-butyl —H J525 (aand b) NH —CF₃ -iso-propyl —H J526 (a and b) NH —CF₃ —CH₃ —CH₃ J527 (aand b) NH —CF₃ —H —H J528 (a and b) NH —CF₃ —H —Cl J529 (a and b) NH—CF₃ —H —Br J530 (a and b) NH —CF₃ —H —F J531 (a and b) NH —CF₃ —H —CH₃J532 (a and b) NH —CF₃ —H —CF₃ J533 (a and b) NH —CF₃ —H —OCH₃ J534 (aand b) NH —CF₃ —H —OCH₂CH₃ J535 (a and b) NH —CF₃ —H —OCF₃ J536 (a andb) NH —CF₃ —H -tert-butyl J537 (a and b) NH —CF₃ —H -iso-propyl J538 (aand b) NH —CHF₂ —Cl —H J539 (a and b) NH —CHF₂ —Br —H J540 (a and b) NH—CHF₂ —F —H J541 (a and b) NH —CHF₂ —CH₃ —H J542 (a and b) NH —CHF₂ —CF₃—H J543 (a and b) NH —CHF₂ —OCH₃ —H J544 (a and b) NH —CHF₂ —OCH₂CH₃ —HJ545 (a and b) NH —CHF₂ —OCF₃ —H J546 (a and b) NH —CHF₂ -tert-butyl —HJ547 (a and b) NH —CHF₂ -iso-propyl —H J548 (a and b) NH —CHF₂ —CH₃ —CH₃J549 (a and b) NH —CHF₂ —H —H J550 (a and b) NH —CHF₂ —H —Cl J551 (a andb) NH —CHF₂ —H —Br J552 (a and b) NH —CHF₂ —H —F J553 (a and b) NH —CHF₂—H —CH₃ J554 (a and b) NH —CHF₂ —H —CF₃ J555 (a and b) NH —CHF₂ —H —OCH₃J556 (a and b) NH —CHF₂ —H —OCH₂CH₃ J557 (a and b) NH —CHF₂ —H —OCF₃J558 (a and b) NH —CHF₂ —H -tert-butyl J559 (a and b) NH —CHF₂ —H-iso-propyl J560 (a and b) NH —OH —Cl —H J561 (a and b) NH —OH —Br —HJ562 (a and b) NH —OH —F —H J563 (a and b) NH —OH —CH₃ —H J564 (a and b)NH —OH —CF₃ —H J565 (a and b) NH —OH —OCH₃ —H J566 (a and b) NH —OH—OCH₂CH₃ —H J567 (a and b) NH —OH —OCF₃ —H J568 (a and b) NH —OH-tert-butyl —H J569 (a and b) NH —OH -iso-propyl —H J570 (a and b) NH—OH —CH₃ —CH₃ J571 (a and b) NH —OH —H —H J572 (a and b) NH —OH —H —ClJ573 (a and b) NH —OH —H —Br J574 (a and b) NH —OH —H —F J575 (a and b)NH —OH —H —CH₃ J576 (a and b) NH —OH —H —CF₃ J577 (a and b) NH —OH —H—OCH₃ J578 (a and b) NH —OH —H —OCH₂CH₃ J579 (a and b) NH —OH —H —OCF₃J580 (a and b) NH —OH —H -tert-butyl J581 (a and b) NH —OH —H-iso-propyl J582 (a and b) NH —NO₂ —Cl —H J583 (a and b) NH —NO₂ —Br —HJ584 (a and b) NH —NO₂ —F —H J585 (a and b) NH —NO₂ —CH₃ —H J586 (a andb) NH —NO₂ —CF₃ —H J587 (a and b) NH —NO₂ —OCH₃ —H J588 (a and b) NH—NO₂ —OCH₂CH₃ —H J589 (a and b) NH —NO₂ —OCF₃ —H J590 (a and b) NH —NO₂-tert-butyl —H J591 (a and b) NH —NO₂ -iso-propyl —H J592 (a and b) NH—NO₂ —CH₃ —CH₃ J593 (a and b) NH —NO₂ —H —H J594 (a and b) NH —NO₂ —H—Cl J595 (a and b) NH —NO₂ —H —Br J596 (a and b) NH —NO₂ —H —F J597 (aand b) NH —NO₂ —H —CH₃ J598 (a and b) NH —NO₂ —H —CF₃ J599 (a and b) NH—NO₂ —H —OCH₃ J600 (a and b) NH —NO₂ —H —OCH₂CH₃ J601 (a and b) NH —NO₂—H —OCF₃ J602 (a and b) NH —NO₂ —H -tert-butyl J603 (a and b) NH —NO₂ —H-iso-propyl J604 (a and b) NH —CN —Br —H J605 (a and b) NH —CN —Cl —HJ606 (a and b) NH —CN —F —H J607 (a and b) NH —CN —CH₃ —H J608 (a and b)NH —CN —CF₃ —H J609 (a and b) NH —CN —OCH₃ —H J610 (a and b) NH —CN—OCH₂CH₃ —H J611 (a and b) NH —CN —OCF₃ —H J612 (a and b) NH —CN-tert-butyl —H J613 (a and b) NH —CN -iso-propyl —H J614 (a and b) NH—CN —CH₃ —CH₃ J615 (a and b) NH —CN —H —H J616 (a and b) NH —CN —H —ClJ617 (a and b) NH —CN —H —Br J618 (a and b) NH —CN —H —F J619 (a and b)NH —CN —H —CH₃ J620 (a and b) NH —CN —H —CF₃ J621 (a and b) NH —CN —H—OCH₃ J622 (a and b) NH —CN —H —OCH₂CH₃ J623 (a and b) NH —CN —H —OCF₃J624 (a and b) NH —CN —H -tert-butyl J625 (a and b) NH —CN —H-iso-propyl J626 (a and b) NH —Br —Br —H J627 (a and b) NH —Br —Cl —HJ628 (a and b) NH —Br —F —H J629 (a and b) NH —Br —CH₃ —H J630 (a and b)NH —Br —CF₃ —H J631 (a and b) NH —Br —OCH₃ —H J632 (a and b) NH —Br—OCH₂CH₃ —H J633 (a and b) NH —Br —OCF₃ —H J634 (a and b) NH —Br-tert-butyl —H J635 (a and b) NH —Br -iso-propyl —H J636 (a and b) NH—Br —CH₃ —CH₃ J637 (a and b) NH —Br —H —H J638 (a and b) NH —Br —H —ClJ639 (a and b) NH —Br —H —Br J640 (a and b) NH —Br —H —F J641 (a and b)NH —Br —H —CH₃ J642 (a and b) NH —Br —H —CF₃ J643 (a and b) NH —Br —H—OCH₃ J644 (a and b) NH —Br —H —OCH₂CH₃ J645 (a and b) NH —Br —H —OCF₃J646 (a and b) NH —Br —H -tert-butyl J647 (a and b) NH —Br —H-iso-propyl J648 (a and b) NH —I —Cl —H J649 (a and b) NH —I —Br —H J650(a and b) NH —I —F —H J651 (a and b) NH —I —CH₃ —H J652 (a and b) NH —I—CF₃ —H J653 (a and b) NH —I —OCH₃ —H J654 (a and b) NH —I —OCH₂CH₃ —HJ655 (a and b) NH —I —OCF₃ —H J656 (a and b) NH —I -tert-butyl —H J657(a and b) NH —I -iso-propyl —H J658 (a and b) NH —I —CH₃ —CH₃ J659 (aand b) NH —I —H —H J660 (a and b) NH —I —H —Cl J661 (a and b) NH —I —H—Br J662 (a and b) NH —I —H —F J663 (a and b) NH —I —H —CH₃ J664 (a andb) NH —I —H —CF₃ J665 (a and b) NH —I —H —OCH₃ J666 (a and b) NH —I —H—OCH₂CH₃ J667 (a and b) NH —I —H —OCF₃ J668 (a and b) NH —I —H-tert-butyl J669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 11 (Ik)

and pharmaceutically acceptable salts thereof, wherein: Compound Ar¹  K1(a and b) -2-(3-chloropyridyl)  K2 (a and b) -2-(3-fluoropyridyl)  K3 (aand b) -2-(3-methylpyridyl)  K4 (a and b) -2-(3-CF₃-pyridyl)  K5 (a andb) -2-(3-CHF₂-pyridyl)  K6 (a and b) -2-(3-hydroxypyridyl)  K7 (a and b)-2-(3-nitropyridyl)  K8 (a and b) -2-(3-cyanopyridyl)  K9 (a and b)-2-(3-bromopyridyl) K10 (a and b) -2-(3-iodopyridyl) K11 (a and b)-4-(5-chloropyrimidinyl) K12 (a and b) -4-(5-methylpyrimidinyl) K13 (aand b) -4-(5-fluoropyrimidinyl) K14 (a and b) -2-(3-chloropyrazinyl) K15(a and b) -2-(3-methylpyrazinyl) K16 (a and b) -2-(3-fluoropyrazinyl)K17 (a and b) -3-(4-chloropyridazinyl) K18 (a and b)-3-(4-methylpyridazinyl) K19 (a and b) -3-(4-fluoropyridazinyl) K20 (aand b) -5-(4-chlorothiadiazolyl) K21 (a and b) -5-(4-methylthiadiazolyl)K22 (a and b) -5-(4-fluorothiadiazolyl) (a) means that R₃ is —H. (b)means that R₃ is —CH₃.

TABLE 12 (Il)

and pharmaceutically acceptable salts thereof, wherein: Compound Ar¹R_(8a) R_(8b)  L1 (a and b) -2-(3-chloropyridyl) —Cl —CF₃  L2 (a and b)-2-(3-chloropyridyl) —CF₃ —Cl  L3 (a and b) -2-(3-chloropyridyl) —CH₃—CF₃  L4 (a and b) -2-(3-chloropyridyl) —SCF₃ —Cl  L5 (a and b)-2-(3-chloropyridyl) —F —CF₃  L6 (a and b) -2-(3-chloropyridyl) —CF₃ —F L7 (a and b) -2-(3-chloropyridyl) —CN —CF₃  L8 (a and b)-2-(3-chloropyridyl) —OCF₃ —Cl  L9 (a and b) -2-(3-fluoropyridyl) —Cl—CF₃  L10 (a and b) -2-(3-fluoropyridyl) —CF₃ —Cl  L11 (a and b)-2-(3-fluoropyridyl) —CH₃ —CF₃  L12 (a and b) -2-(3-fluoropyridyl) —SCF₃—Cl  L13 (a and b) -2-(3-fluoropyridyl) —F —CF₃  L14 (a and b)-2-(3-fluoropyridyl) —CF₃ —F  L15 (a and b) -2-(3-fluoropyridyl) —CN—CF₃  L16 (a and b) -2-(3-fluoropyridyl) —OCF₃ —Cl  L17 (a and b)-2-(3-methylpyridyl) —Cl —CF₃  L18 (a and b) -2-(3-methylpyridyl) —CF₃—Cl  L19 (a and b) -2-(3-methylpyridyl) —CH₃ —CF₃  L20 (a and b)-2-(3-methylpyridyl) —SCF₃ —Cl  L21 (a and b) -2-(3-methylpyridyl) —F—CF₃  L22 (a and b) -2-(3-methylpyridyl) —CF₃ —F  L23 (a and b)-2-(3-methylpyridyl) —CN —CF₃  L24 (a and b) -2-(3-methylpyridyl) —OCF₃—Cl  L25 (a and b) -2-(3-CF₃-pyridyl) —Cl —CF₃  L26 (a and b)-2-(3-CF₃-pyridyl) —CF₃ —Cl  L27 (a and b) -2-(3-CF₃-pyridyl) —CH₃ —CF₃ L28 (a and b) -2-(3-CF₃-pyridyl) —SCF₃ —Cl  L29 (a and b)-2-(3-CF₃-pyridyl) —F —CF₃  L30 (a and b) -2-(3-CF₃-pyridyl) —CF₃ —F L31 (a and b) -2-(3-CF₃-pyridyl) —CN —CF₃  L32 (a and b)-2-(3-CF₃-pyridyl) —OCF₃ —Cl  L33 (a and b) -2-(3-CHF₂-pyridyl) —Cl —CF₃ L34 (a and b) -2-(3-CHF₂-pyridyl) —CF₃ —Cl  L35 (a and b)-2-(3-CHF₂-pyridyl) —CH₃ —CF₃  L36 (a and b) -2-(3-CHF₂-pyridyl) —SCF₃—Cl  L37 (a and b) -2-(3-CHF₂-pyridyl) —F —CF₃  L38 (a and b)-2-(3-CHF₂-pyridyl) —CF₃ —F  L39 (a and b) -2-(3-CHF₂-pyridyl) —CN —CF₃ L40 (a and b) -2-(3-CHF₂-pyridyl) —OCF₃ —Cl  L41 (a and b)-2-(3-hydroxypyridyl) —Cl —CF₃  L42 (a and b) -2-(3-hydroxypyridyl) —CF₃—Cl  L43 (a and b) -2-(3-hydroxypyridyl) —CH₃ —CF₃  L44 (a and b)-2-(3-hydroxypyridyl) —SCF₃ —Cl  L45 (a and b) -2-(3-hydroxypyridyl) —F—CF₃  L46 (a and b) -2-(3-hydroxypyridyl) —CF₃ —F  L47 (a and b)-2-(3-hydroxypyridyl) —CN —CF₃  L48 (a and b) -2-(3-hydroxypyridyl)—OCF₃ —Cl  L49 (a and b) -2-(3-nitropyridyl) —Cl —CF₃  L50 (a and b)-2-(3-nitropyridyl) —CF₃ —Cl  L51 (a and b) -2-(3-nitropyridyl) —CH₃—CF₃  L52 (a and b) -2-(3-nitropyridyl) —SCF₃ —Cl  L53 (a and b)-2-(3-nitropyridyl) —F —CF₃  L54 (a and b) -2-(3-nitropyridyl) —CF₃ —F L55 (a and b) -2-(3-nitropyridyl) —CN —CF₃  L56 (a and b)-2-(3-nitropyridyl) —OCF₃ —Cl  L57 (a and b) -2-(3-cyanopyridyl) —Cl—CF₃  L58 (a and b) -2-(3-cyanopyridyl) —CF₃ —Cl  L59 (a and b)-2-(3-cyanopyridyl) —CH₃ —CF₃  L60 (a and b) -2-(3-cyanopyridyl) —SCF₃—Cl  L61 (a and b) -2-(3-cyanopyridyl) —F —CF₃  L62 (a and b)-2-(3-cyanopyridyl) —CF₃ —F  L63 (a and b) -2-(3-cyanopyridyl) —CN —CF₃ L64 (a and b) -2-(3-cyanopyridyl) —OCF₃ —Cl  L65 (a and b)-2-(3-bromopyridyl) —Cl —CF₃  L66 (a and b) -2-(3-bromopyridyl) —CF₃ —Cl L67 (a and b) -2-(3-bromopyridyl) —CH₃ —CF₃  L68 (a and b)-2-(3-bromopyridyl) —SCF₃ —Cl  L69 (a and b) -2-(3-bromopyridyl) —F —CF₃ L70 (a and b) -2-(3-bromopyridyl) —CF₃ —F  L71 (a and b)-2-(3-bromopyridyl) —CN —CF₃  L72 (a and b) -2-(3-bromopyridyl) —OCF₃—Cl  L73 (a and b) -2-(3-iodopyridyl) —Cl —CF₃  L74 (a and b)-2-(3-iodopyridyl) —CF₃ —Cl  L75 (a and b) -2-(3-iodopyridyl) —CH₃ —CF₃ L76 (a and b) -2-(3-iodopyridyl) —SCF₃ —Cl  L77 (a and b)-2-(3-iodopyridyl) —F —CF₃  L78 (a and b) -2-(3-iodopyridyl) —CF₃ —F L79 (a and b) -2-(3-iodopyridyl) —CN —CF₃  L80 (a and b)-2-(3-iodopyridyl) —OCF₃ —Cl  L81 (a and b) -4-(5-chloropyrimidinyl) —Cl—CF₃  L82 (a and b) -4-(5-chloropyrimidinyl) —CF₃ —Cl  L83 (a and b)-4-(5-chloropyrimidinyl) —CH₃ —CF₃  L84 (a and b)-4-(5-chloropyrimidinyl) —SCF₃ —Cl  L85 (a and b)-4-(5-chloropyrimidinyl) —F —CF₃  L86 (a and b) -4-(5-chloropyrimidinyl)—CF₃ —F  L87 (a and b) -4-(5-chloropyrimidinyl) —CN —CF₃  L88 (a and b)-4-(5-chloropyrimidinyl) —OCF₃ —Cl  L89 (a and b)-4-(5-methylpyrimidinyl) —Cl —CF₃  L90 (a and b)-4-(5-methylpyrimidinyl) —CF₃ —Cl  L91 (a and b)-4-(5-methylpyrimidinyl) —CH₃ —CF₃  L92 (a and b)-4-(5-methylpyrimidinyl) —SCF₃ —Cl  L93 (a and b)-4-(5-methylpyrimidinyl) —F —CF₃  L94 (a and b) -4-(5-methylpyrimidinyl)—CF₃ —F  L95 (a and b) -4-(5-methylpyrimidinyl) —CN —CF₃  L96 (a and b)-4-(5-methylpyrimidinyl) —OCF₃ —Cl  L97 (a and b)-4-(5-fluoropyrimidinyl) —Cl —CF₃  L98 (a and b)-4-(5-fluoropyrimidinyl) —CF₃ —Cl  L99 (a and b)-4-(5-fluoropyrimidinyl) —CH₃ —CF₃ L100 (a and b)-4-(5-fluoropyrimidinyl) —SCF₃ —Cl L101 (a and b)-4-(5-fluoropyrimidinyl) —F —CF₃ L102 (a and b) -4-(5-fluoropyrimidinyl)—CF₃ —F L103 (a and b) -4-(5-fluoropyrimidinyl) —CN —CF₃ L104 (a and b)-4-(5-fluoropyrimidinyl) —OCF₃ —Cl L105 (a and b) -2-(3-chloropyrazinyl)—Cl —CF₃ L106 (a and b) -2-(3-chloropyrazinyl) —CF₃ —Cl L107 (a and b)-2-(3-chloropyrazinyl) —CH₃ —CF₃ L108 (a and b) -2-(3-chloropyrazinyl)—SCF₃ —Cl L109 (a and b) -2-(3-chloropyrazinyl) —F —CF₃ L110 (a and b)-2-(3-chloropyrazinyl) —CF₃ —F L111 (a and b) -2-(3-chloropyrazinyl) —CN—CF₃ L112 (a and b) -2-(3-chloropyrazinyl) —OCF₃ —Cl L113 (a and b)-2-(3-methylpyrazinyl) —Cl —CF₃ L114 (a and b) -2-(3-methylpyrazinyl)—CF₃ —Cl L115 (a and b) -2-(3-methylpyrazinyl) —CH₃ —CF₃ L116 (a and b)-2-(3-methylpyrazinyl) —SCF₃ —Cl L117 (a and b) -2-(3-methylpyrazinyl)—F —CF₃ L118 (a and b) -2-(3-methylpyrazinyl) —CF₃ —F L119 (a and b)-2-(3-methylpyrazinyl) —CN —CF₃ L120 (a and b) -2-(3-methylpyrazinyl)—OCF₃ —Cl L121 (a and b) -2-(3-fluoropyrazinyl) —Cl —CF₃ L122 (a and b)-2-(3-fluoropyrazinyl) —CF₃ —Cl L123 (a and b) -2-(3-fluoropyrazinyl)—CH₃ —CF₃ L124 (a and b) -2-(3-fluoropyrazinyl) —SCF₃ —Cl L125 (a and b)-2-(3-fluoropyrazinyl) —F —CF₃ L126 (a and b) -2-(3-fluoropyrazinyl)—CF₃ —F L127 (a and b) -2-(3-fluoropyrazinyl) —CN —CF₃ L128 (a and b)-2-(3-fluoropyrazinyl) —OCF₃ —Cl L129 (a and b) -3-(4-chloropyridazinyl)—Cl —CF₃ L130 (a and b) -3-(4-chloropyridazinyl) —CF₃ —Cl L131 (a and b)-3-(4-chloropyridazinyl) —CH₃ —CF₃ L132 (a and b)-3-(4-chloropyridazinyl) —SCF₃ —Cl L133 (a and b)-3-(4-chloropyridazinyl) —F —CF₃ L134 (a and b) -3-(4-chloropyridazinyl)—CF₃ —F L135 (a and b) -3-(4-chloropyridazinyl) —CN —CF₃ L136 (a and b)-3-(4-chloropyridazinyl) —OCF₃ —Cl L137 (a and b)-3-(4-methylpyridazinyl) —Cl —CF₃ L138 (a and b)-3-(4-methylpyridazinyl) —CF₃ —Cl L139 (a and b)-3-(4-methylpyridazinyl) —CH₃ —CF₃ L140 (a and b)-3-(4-methylpyridazinyl) —SCF₃ —Cl L141 (a and b)-3-(4-methylpyridazinyl) —F —CF₃ L142 (a and b) -3-(4-methylpyridazinyl)—CF₃ —F L143 (a and b) -3-(4-methylpyridazinyl) —CN —CF₃ L144 (a and b)-3-(4-methylpyridazinyl) —OCF₃ —Cl L145 (a and b)-3-(4-fluoropyridazinyl) —Cl —CF₃ L146 (a and b)-3-(4-fluoropyridazinyl) —CF₃ —Cl L147 (a and b)-3-(4-fluoropyridazinyl) —CH₃ —CF₃ L148 (a and b)-3-(4-fluoropyridazinyl) —SCF₃ —Cl L149 (a and b)-3-(4-fluoropyridazinyl) —F —CF₃ L150 (a and b) -3-(4-fluoropyridazinyl)—CF₃ —F L151 (a and b) -3-(4-fluoropyridazinyl) —CN —CF₃ L152 (a and b)-3-(4-fluoropyridazinyl) —OCF₃ —Cl L153 (a and b)-5-(4-chlorothiadiazolyl) —Cl —CF₃ L154 (a and b)-5-(4-chlorothiadiazolyl) —CF₃ —Cl L155 (a and b)-5-(4-chlorothiadiazolyl) —CH₃ —CF₃ L156 (a and b)-5-(4-chlorothiadiazolyl) —SCF₃ —Cl L157 (a and b)-5-(4-chlorothiadiazolyl) —F —CF₃ L158 (a and b)-5-(4-chlorothiadiazolyl) —CF₃ —F L159 (a and b)-5-(4-chlorothiadiazolyl) —CN —CF₃ L160 (a and b)-5-(4-chlorothiadiazolyl) —OCF₃ —Cl L161 (a and b)-5-(4-methylthiadiazolyl) —Cl —CF₃ L162 (a and b)-5-(4-methylthiadiazolyl) —CF₃ —Cl L163 (a and b)-5-(4-methylthiadiazolyl) —CH₃ —CF₃ L164 (a and b)-5-(4-methylthiadiazolyl) —SCF₃ —Cl L165 (a and b)-5-(4-methylthiadiazolyl) —F —CF₃ L166 (a and b)-5-(4-methylthiadiazolyl) —CF₃ —F L167 (a and b)-5-(4-methylthiadiazolyl) —CN —CF₃ L168 (a and b)-5-(4-methylthiadiazolyl) —OCF₃ —Cl L169 (a and b)-5-(4-fluorothiadiazolyl) —Cl —CF₃ L170 (a and b)-5-(4-fluorothiadiazolyl) —CF₃ —Cl L171 (a and b)-5-(4-fluorothiadiazolyl) —CH₃ —CF₃ L172 (a and b)-5-(4-fluorothiadiazolyl) —SCF₃ —Cl L173 (a and b)-5-(4-fluorothiadiazolyl) —F —CF₃ L174 (a and b)-5-(4-fluorothiadiazolyl) —CF₃ —F L175 (a and b)-5-(4-fluorothiadiazolyl) —CN —CF₃ L176 (a and b)-5-(4-fluorothiadiazolyl) —OCF₃ —Cl (a) means that R₃ is —H. (b) meansthat R₃ is —CH₃.

TABLE 13 (Im)

and pharmaceutically acceptable salts thereof, wherein: Compound Ar¹ Z₁Z₂ R_(8a)  M1 (a and b) -2-(3-chloropyridyl) N CH —CF₃  M2 (a and b)-2-(3-fluoropyridyl) N CH —CF₃  M3 (a and b) -2-(3-methylpyridyl) N CH—CF₃  M4 (a and b) -2-(3-CF₃-pyridyl) N CH —CF₃  M5 (a and b)-2-(3-CHF₂-pyridyl) N CH —CF₃  M6 (a and b) -2-(3-hydroxypyridyl) N CH—CF₃  M7 (a and b) -2-(3-nitropyridyl) N CH —CF₃  M8 (a and b)-2-(3-cyanopyridyl) N CH —CF₃  M9 (a and b) -2-(3-bromopyridyl) N CH—CF₃  M10 (a and b) -2-(3-iodopyridyl) N CH —CF₃  M11 (a and b)-4-(5-chloropyrimidinyl) N CH —CF₃  M12 (a and b)-4-(5-methylpyrimidinyl) N CH —CF₃  M13 (a and b)-4-(5-fluoropyrimidinyl) N CH —CF₃  M14 (a and b) -2-(3-chloropyrazinyl)N CH —CF₃  M15 (a and b) -2-(3-methylpyrazinyl) N CH —CF₃  M16 (a and b)-2-(3-fluoropyrazinyl) N CH —CF₃  M17 (a and b) -3-(4-chloropyridazinyl)N CH —CF₃  M18 (a and b) -3-(4-methylpyridazinyl) N CH —CF₃  M19 (a andb) -3-(4-fluoropyridazinyl) N CH —CF₃  M20 (a and b)-5-(4-chlorothiadiazolyl) N CH —CF₃  M21 (a and b)-5-(4-methylthiadiazolyl) N N —CF₃  M22 (a and b)-5-(4-fluorothiadiazolyl) N CH —CF₃  M23 (a and b) -2-(3-chloropyridyl)CH N —CF₃  M24 (a and b) -2-(3-fluoropyridyl) CH N —CF₃  M25 (a and b)-2-(3-methylpyridyl) CH N —CF₃  M26 (a and b) -2-(3-CF₃-pyridyl) CH N—CF₃  M27 (a and b) -2-(3-CHF₂-pyridyl) CH N —CF₃  M28 (a and b)-2-(3-hydroxypyridyl) CH N —CF₃  M29 (a and b) -2-(3-nitropyridyl) CH N—CF₃  M30 (a and b) -2-(3-cyanopyridyl) CH N —CF₃  M31 (a and b)-2-(3-bromopyridyl) CH N —CF₃  M32 (a and b) -2-(3-iodopyridyl) CH N—CF₃  M33 (a and b) -4-(5-chloropyrimidinyl) CH N —CF₃  M34 (a and b)-4-(5-methylpyrimidinyl) CH N —CF₃  M35 (a and b)-4-(5-fluoropyrimidinyl) CH N —CF₃  M36 (a and b) -2-(3-chloropyrazinyl)CH N —CF₃  M37 (a and b) -2-(3-methylpyrazinyl) CH N —CF₃  M38 (a and b)-2-(3-fluoropyrazinyl) CH N —CF₃  M39 (a and b) -3-(4-chloropyridazinyl)CH N —CF₃  M40 (a and b) -3-(4-methylpyridazinyl) CH N —CF₃  M41 (a andb) -3-(4-fluoropyridazinyl) CH N —CF₃  M42 (a and b)-5-(4-chlorothiadiazolyl) CH N —CF₃  M43 (a and b)-5-(4-methylthiadiazolyl) N N —CF₃  M44 (a and b)-5-(4-fluorothiadiazolyl) CH N —CF₃  M45 (a and b) -2-(3-chloropyridyl)N CH -tert-butyl  M46 (a and b) -2-(3-fluoropyridyl) N CH -tert-butyl M47 (a and b) -2-(3-methylpyridyl) N CH -tert-butyl  M48 (a and b)-2-(3-CF₃-pyridyl) N CH -tert-butyl  M49 (a and b) -2-(3-CHF₂-pyridyl) NCH -tert-butyl  M50 (a and b) -2-(3-hydroxypyridyl) N CH -tert-butyl M51 (a and b) -2-(3-nitropyridyl) N CH -tert-butyl  M52 (a and b)-2-(3-cyanopyridyl) N CH -tert-butyl  M53 (a and b) -2-(3-bromopyridyl)N CH -tert-butyl  M54 (a and b) -2-(3-iodopyridyl) N CH -tert-butyl  M55(a and b) -4-(5-chloropyrimidinyl) N CH -tert-butyl  M56 (a and b)-4-(5-methylpyrimidinyl) N CH -tert-butyl  M57 (a and b)-4-(5-fluoropyrimidinyl) N CH -tert-butyl  M58 (a and b)-2-(3-chloropyrazinyl) N CH -tert-butyl  M59 (a and b)-2-(3-methylpyrazinyl) N CH -tert-butyl  M60 (a and b)-2-(3-fluoropyrazinyl) N CH -tert-butyl  M61 (a and b)-3-(4-chloropyridazinyl) N CH -tert-butyl  M62 (a and b)-3-(4-methylpyridazinyl) N CH -tert-butyl  M63 (a and b)-3-(4-fluoropyridazinyl) N CH -tert-butyl  M64 (a and b)-5-(4-chlorothiadiazolyl) N CH -tert-butyl  M65 (a and b)-5-(4-methylthiadiazolyl) N N -tert-butyl  M66 (a and b)-5-(4-fluorothiadiazolyl) N CH -tert-butyl  M67 (a and b)-2-(3-chloropyridyl) CH N -tert-butyl  M68 (a and b)-2-(3-fluoropyridyl) CH N -tert-butyl  M69 (a and b)-2-(3-methylpyridyl) CH N -tert-butyl  M70 (a and b) -2-(3-CF₃-pyridyl)CH N -tert-butyl  M71 (a and b) -2-(3-CHF₂-pyridyl) CH N -tert-butyl M72 (a and b) -2-(3-hydroxypyridyl) CH N -tert-butyl  M73 (a and b)-2-(3-nitropyridyl) CH N -tert-butyl  M74 (a and b) -2-(3-cyanopyridyl)CH N -tert-butyl  M75 (a and b) -2-(3-bromopyridyl) CH N -tert-butyl M76 (a and b) -2-(3-iodopyridyl) CH N -tert-butyl  M77 (a and b)-4-(5-chloropyrimidinyl) CH N -tert-butyl  M78 (a and b)-4-(5-methylpyrimidinyl) CH N -tert-butyl  M79 (a and b)-4-(5-fluoropyrimidinyl) CH N -tert-butyl  M80 (a and b)-2-(3-chloropyrazinyl) CH N -tert-butyl  M81 (a and b)-2-(3-methylpyrazinyl) CH N -tert-butyl  M82 (a and b)-2-(3-fluoropyrazinyl) CH N -tert-butyl  M83 (a and b)-3-(4-chloropyridazinyl) CH N -tert-butyl  M84 (a and b)-3-(4-methylpyridazinyl) CH N -tert-butyl  M85 (a and b)-3-(4-fluoropyridazinyl) CH N -tert-butyl  M86 (a and b)-5-(4-chlorothiadiazolyl) CH N -tert-butyl  M87 (a and b)-5-(4-methylthiadiazolyl) N N -tert-butyl  M88 (a and b)-5-(4-fluorothiadiazolyl) CH N -tert-butyl  M89 (a and b)-2-(3-chloropyridyl) N CH -iso-butyl  M90 (a and b) -2-(3-fluoropyridyl)N CH -iso-butyl  M91 (a and b) -2-(3-methylpyridyl) N CH -iso-butyl  M92(a and b) -2-(3-CF₃-pyridyl) N CH -iso-butyl  M93 (a and b)-2-(3-CHF₂-pyridyl) N CH -iso-butyl  M94 (a and b) -2-(3-hydroxypyridyl)N CH -iso-butyl  M95 (a and b) -2-(3-nitropyridyl) N CH -iso-butyl  M96(a and b) -2-(3-cyanopyridyl) N CH -iso-butyl  M97 (a and b)-2-(3-bromopyridyl) N CH -iso-butyl  M98 (a and b) -2-(3-iodopyridyl) NCH -iso-butyl  M99 (a and b) -4-(5-chloropyrimidinyl) N CH -iso-butylM100 (a and b) -4-(5-methylpyrimidinyl) N CH -iso-butyl M101 (a and b)-4-(5-fluoropyrimidinyl) N CH -iso-butyl M102 (a and b)-2-(3-chloropyrazinyl) N CH -iso-butyl M103 (a and b)-2-(3-methylpyrazinyl) N CH -iso-butyl M104 (a and b)-2-(3-fluoropyrazinyl) N CH -iso-butyl M105 (a and b)-3-(4-chloropyridazinyl) N CH -iso-butyl M106 (a and b)-3-(4-methylpyridazinyl) N CH -iso-butyl M107 (a and b)-3-(4-fluoropyridazinyl) N CH -iso-butyl M108 (a and b)-5-(4-chlorothiadiazolyl) N CH -iso-butyl M109 (a and b)-5-(4-methylthiadiazolyl) N N -iso-butyl M110 (a and b)-5-(4-fluorothiadiazolyl) N CH -iso-butyl M111 (a and b)-2-(3-chloropyridyl) CH N -iso-butyl M112 (a and b) -2-(3-fluoropyridyl)CH N -iso-butyl M113 (a and b) -2-(3-methylpyridyl) CH N -iso-butyl M114(a and b) -2-(3-CF₃-pyridyl) CH N -iso-butyl M115 (a and b)-2-(3-CHF₂-pyridyl) CH N -iso-butyl M116 (a and b) -2-(3-hydroxypyridyl)CH N -iso-butyl M117 (a and b) -2-(3-nitropyridyl) CH N -iso-butyl M118(a and b) -2-(3-cyanopyridyl) CH N -iso-butyl M119 (a and b)-2-(3-bromopyridyl) CH N -iso-butyl M120 (a and b) -2-(3-iodopyridyl) CHN -iso-butyl M121 (a and b) -4-(5-chloropyrimidinyl) CH N -iso-butylM122 (a and b) -4-(5-methylpyrimidinyl) CH N -iso-butyl M123 (a and b)-4-(5-fluoropyrimidinyl) CH N -iso-butyl M124 (a and b)-2-(3-chloropyrazinyl) CH N -iso-butyl M125 (a and b)-2-(3-methylpyrazinyl) CH N -iso-butyl M126 (a and b)-2-(3-fluoropyrazinyl) CH N -iso-butyl M127 (a and b)-3-(4-chloropyridazinyl) CH N -iso-butyl M128 (a and b)-3-(4-methylpyridazinyl) CH N -iso-butyl M129 (a and b)-3-(4-fluoropyridazinyl) CH N -iso-butyl M130 (a and b)-5-(4-chlorothiadiazolyl) CH N -iso-butyl M131 (a and b)-5-(4-methylthiadiazolyl) N N -iso-butyl M132 (a and b)-5-(4-fluorothiadiazolyl) CH N -iso-butyl M133 (a and b)-2-(3-chloropyridyl) N CH -sec-butyl M134 (a and b) -2-(3-fluoropyridyl)N CH -sec-butyl M135 (a and b) -2-(3-methylpyridyl) N CH -sec-butyl M136(a and b) -2-(3-CF₃-pyridyl) N CH -sec-butyl M137 (a and b)-2-(3-CHF₂-pyridyl) N CH -sec-butyl M138 (a and b) -2-(3-hydroxypyridyl)N CH -sec-butyl M139 (a and b) -2-(3-nitropyridyl) N CH -sec-butyl M140(a and b) -2-(3-cyanopyridyl) N CH -sec-butyl M141 (a and b)-2-(3-bromopyridyl) N CH -sec-butyl M142 (a and b) -2-(3-iodopyridyl) NCH -sec-butyl M143 (a and b) -4-(5-chloropyrimidinyl) N CH -sec-butylM144 (a and b) -4-(5-methylpyrimidinyl) N CH -sec-butyl M145 (a and b)-4-(5-fluoropyrimidinyl) N CH -sec-butyl M146 (a and b)-2-(3-chloropyrazinyl) N CH -sec-butyl M147 (a and b)-2-(3-methylpyrazinyl) N CH -sec-butyl M148 (a and b)-2-(3-fluoropyrazinyl) N CH -sec-butyl M149 (a and b)-3-(4-chloropyridazinyl) N CH -sec-butyl M150 (a and b)-3-(4-methylpyridazinyl) N CH -sec-butyl M151 (a and b)-3-(4-fluoropyridazinyl) N CH -sec-butyl M152 (a and b)-5-(4-chlorothiadiazolyl) N CH -sec-butyl M153 (a and b)-5-(4-methylthiadiazolyl) N N -sec-butyl M154 (a and b)-5-(4-fluorothiadiazolyl) N CH -sec-butyl M155 (a and b)-2-(3-chloropyridyl) CH N -sec-butyl M156 (a and b) -2-(3-fluoropyridyl)CH N -sec-butyl M157 (a and b) -2-(3-methylpyridyl) CH N -sec-butyl M158(a and b) -2-(3-CF₃-pyridyl) CH N -sec-butyl M159 (a and b)-2-(3-CHF₂-pyridyl) CH N -sec-butyl M160 (a and b) -2-(3-hydroxypyridyl)CH N -sec-butyl M161 (a and b) -2-(3-nitropyridyl) CH N -sec-butyl M162(a and b) -2-(3-cyanopyridyl) CH N -sec-butyl M163 (a and b)-2-(3-bromopyridyl) CH N -sec-butyl M164 (a and b) -2-(3-iodopyridyl) CHN -sec-butyl M165 (a and b) -4-(5-chloropyrimidinyl) CH N -sec-butylM166 (a and b) -4-(5-methylpyrimidinyl) CH N -sec-butyl M167 (a and b)-4-(5-fluoropyrimidinyl) CH N -sec-butyl M168 (a and b)-2-(3-chloropyrazinyl) CH N -sec-butyl M169 (a and b)-2-(3-methylpyrazinyl) CH N -sec-butyl M170 (a and b)-2-(3-fluoropyrazinyl) CH N -sec-butyl M171 (a and b)-3-(4-chloropyridazinyl) CH N -sec-butyl M172 (a and b)-3-(4-methylpyridazinyl) CH N -sec-butyl M173 (a and b)-3-(4-fluoropyridazinyl) CH N -sec-butyl M174 (a and b)-5-(4-chlorothiadiazolyl) CH N -sec-butyl M175 (a and b)-5-(4-methylthiadiazolyl) N N -sec-butyl M176 (a and b)-5-(4-fluorothiadiazolyl) CH N -sec-butyl M177 (a and b)-2-(3-chloropyridyl) N CH -iso-propyl M178 (a and b)-2-(3-fluoropyridyl) N CH -iso-propyl M179 (a and b)-2-(3-methylpyridyl) N CH -iso-propyl M180 (a and b) -2-(3-CF₃-pyridyl)N CH -iso-propyl M181 (a and b) -2-(3-CHF₂-pyridyl) N CH -iso-propylM182 (a and b) -2-(3-hydroxypyridyl) N CH -iso-propyl M183 (a and b)-2-(3-nitropyridyl) N CH -iso-propyl M184 (a and b) -2-(3-cyanopyridyl)N CH -iso-propyl M185 (a and b) -2-(3-bromopyridyl) N CH -iso-propylM186 (a and b) -2-(3-iodopyridyl) N CH -iso-propyl M187 (a and b)-4-(5-chloropyrimidinyl) N CH -iso-propyl M188 (a and b)-4-(5-methylpyrimidinyl) N CH -iso-propyl M189 (a and b)-4-(5-fluoropyrimidinyl) N CH -iso-propyl M190 (a and b)-2-(3-chloropyrazinyl) N CH -iso-propyl M191 (a and b)-2-(3-methylpyrazinyl) N CH -iso-propyl M192 (a and b)-2-(3-fluoropyrazinyl) N CH -iso-propyl M193 (a and b)-3-(4-chloropyridazinyl) N CH -iso-propyl M194 (a and b)-3-(4-methylpyridazinyl) N CH -iso-propyl M195 (a and b)-3-(4-fluoropyridazinyl) N CH -iso-propyl M196 (a and b)-5-(4-chlorothiadiazolyl) N CH -iso-propyl M197 (a and b)-5-(4-methylthiadiazolyl) N N -iso-propyl M198 (a and b)-5-(4-fluorothiadiazolyl) N CH -iso-propyl M199 (a and b)-2-(3-chloropyridyl) CH N -iso-propyl M200 (a and b)-2-(3-fluoropyridyl) CH N -iso-propyl M201 (a and b)-2-(3-methylpyridyl) CH N -iso-propyl M202 (a and b) -2-(3-CF₃-pyridyl)CH N -iso-propyl M203 (a and b) -2-(3-CHF₂-pyridyl) CH N -iso-propylM204 (a and b) -2-(3-hydroxypyridyl) CH N -iso-propyl M205 (a and b)-2-(3-nitropyridyl) CH N -iso-propyl M206 (a and b) -2-(3-cyanopyridyl)CH N -iso-propyl M207 (a and b) -2-(3-bromopyridyl) CH N -iso-propylM208 (a and b) -2-(3-iodopyridyl) CH N -iso-propyl M209 (a and b)-4-(5-chloropyrimidinyl) CH N -iso-propyl M210 (a and b)-4-(5-methylpyrimidinyl) CH N -iso-propyl M211 (a and b)-4-(5-fluoropyrimidinyl) CH N -iso-propyl M212 (a and b)-2-(3-chloropyrazinyl) CH N -iso-propyl M213 (a and b)-2-(3-methylpyrazinyl) CH N -iso-propyl M214 (a and b)-2-(3-fluoropyrazinyl) CH N -iso-propyl M215 (a and b)-3-(4-chloropyridazinyl) CH N -iso-propyl M216 (a and b)-3-(4-methylpyridazinyl) CH N -iso-propyl M217 (a and b)-3-(4-fluoropyridazinyl) CH N -iso-propyl M218 (a and b)-5-(4-chlorothiadiazolyl) CH N -iso-propyl M219 (a and b)-5-(4-methylthiadiazolyl) N N -iso-propyl M220 (a and b)-5-(4-fluorothiadiazolyl) CH N -iso-propyl M221 (a and b)-2-(3-chloropyridyl) N CH -cyclohexyl M222 (a and b)-2-(3-fluoropyridyl) N CH -cyclohexyl M223 (a and b)-2-(3-methylpyridyl) N CH -cyclohexyl M224 (a and b) -2-(3-CF₃-pyridyl)N CH -cyclohexyl M225 (a and b) -2-(3-CHF₂-pyridyl) N CH -cyclohexylM226 (a and b) -2-(3-hydroxypyridyl) N CH -cyclohexyl M227 (a and b)-2-(3-nitropyridyl) N CH -cyclohexyl M228 (a and b) -2-(3-cyanopyridyl)N CH -cyclohexyl M229 (a and b) -2-(3-bromopyridyl) N CH -cyclohexylM230 (a and b) -2-(3-iodopyridyl) N CH -cyclohexyl M231 (a and b)-4-(5-chloropyrimidinyl) N CH -cyclohexyl M232 (a and b)-4-(5-methylpyrimidinyl) N CH -cyclohexyl M233 (a and b)-4-(5-fluoropyrimidinyl) N CH -cyclohexyl M234 (a and b)-2-(3-chloropyrazinyl) N CH -cyclohexyl M235 (a and b)-2-(3-methylpyrazinyl) N CH -cyclohexyl M236 (a and b)-2-(3-fluoropyrazinyl) N CH -cyclohexyl M237 (a and b)-3-(4-chloropyridazinyl) N CH -cyclohexyl M238 (a and b)-3-(4-methylpyridazinyl) N CH -cyclohexyl M239 (a and b)-3-(4-fluoropyridazinyl) N CH -cyclohexyl M240 (a and b)-5-(4-chlorothiadiazolyl) N CH -cyclohexyl M241 (a and b)-5-(4-methylthiadiazolyl) N N -cyclohexyl M242 (a and b)-5-(4-fluorothiadiazolyl) N CH -cyclohexyl M243 (a and b)-2-(3-chloropyridyl) CH N -cyclohexyl M244 (a and b)-2-(3-fluoropyridyl) CH N -cyclohexyl M245 (a and b)-2-(3-methylpyridyl) CH N -cyclohexyl M246 (a and b) -2-(3-CF₃-pyridyl)CH N -cyclohexyl M247 (a and b) -2-(3-CHF₂-pyridyl) CH N -cyclohexylM248 (a and b) -2-(3-hydroxypyridyl) CH N -cyclohexyl M249 (a and b)-2-(3-nitropyridyl) CH N -cyclohexyl M250 (a and b) -2-(3-cyanopyridyl)CH N -cyclohexyl M251 (a and b) -2-(3-bromopyridyl) CH N -cyclohexylM252 (a and b) -2-(3-iodopyridyl) CH N -cyclohexyl M253 (a and b)-4-(5-chloropyrimidinyl) CH N -cyclohexyl M254 (a and b)-4-(5-methylpyrimidinyl) CH N -cyclohexyl M255 (a and b)-4-(5-fluoropyrimidinyl) CH N -cyclohexyl M256 (a and b)-2-(3-chloropyrazinyl) CH N -cyclohexyl M257 (a and b)-2-(3-methylpyrazinyl) CH N -cyclohexyl M258 (a and b)-2-(3-fluoropyrazinyl) CH N -cyclohexyl M259 (a and b)-3-(4-chloropyridazinyl) CH N -cyclohexyl M260 (a and b)-3-(4-methylpyridazinyl) CH N -cyclohexyl M261 (a and b)-3-(4-fluoropyridazinyl) CH N -cyclohexyl M262 (a and b)-5-(4-chlorothiadiazolyl) CH N -cyclohexyl M263 (a and b)-5-(4-methylthiadiazolyl) N N -cyclohexyl M264 (a and b)-5-(4-fluorothiadiazolyl) CH N -cyclohexyl M265 (a and b)-2-(3-chloropyridyl) N CH —CH₂CF₃ M266 (a and b) -2-(3-fluoropyridyl) NCH —CH₂CF₃ M267 (a and b) -2-(3-methylpyridyl) N CH —CH₂CF₃ M268 (a andb) -2-(3-CF₃-pyridyl) N CH —CH₂CF₃ M269 (a and b) -2-(3-CHF₂-pyridyl) NCH —CH₂CF₃ M270 (a and b) -2-(3-hydroxypyridyl) N CH —CH₂CF₃ M271 (a andb) -2-(3-nitropyridyl) N CH —CH₂CF₃ M272 (a and b) -2-(3-cyanopyridyl) NCH —CH₂CF₃ M273 (a and b) -2-(3-bromopyridyl) N CH —CH₂CF₃ M274 (a andb) -2-(3-iodopyridyl) N CH —CH₂CF₃ M275 (a and b)-4-(5-chloropyrimidinyl) N CH —CH₂CF₃ M276 (a and b)-4-(5-methylpyrimidinyl) N CH —CH₂CF₃ M277 (a and b)-4-(5-fluoropyrimidinyl) N CH —CH₂CF₃ M278 (a and b)-2-(3-chloropyrazinyl) N CH —CH₂CF₃ M279 (a and b)-2-(3-methylpyrazinyl) N CH —CH₂CF₃ M280 (a and b)-2-(3-fluoropyrazinyl) N CH —CH₂CF₃ M281 (a and b)-3-(4-chloropyridazinyl) N CH —CH₂CF₃ M282 (a and b)-3-(4-methylpyridazinyl) N CH —CH₂CF₃ M283 (a and b)-3-(4-fluoropyridazinyl) N CH —CH₂CF₃ M284 (a and b)-5-(4-chlorothiadiazolyl) N CH —CH₂CF₃ M285 (a and b)-5-(4-methylthiadiazolyl) N N —CH₂CF₃ M286 (a and b)-5-(4-fluorothiadiazolyl) N CH —CH₂CF₃ M287 (a and b)-2-(3-chloropyridyl) CH N —CH₂CF₃ M288 (a and b) -2-(3-fluoropyridyl) CHN —CH₂CF₃ M289 (a and b) -2-(3-methylpyridyl) CH N —CH₂CF₃ M290 (a andb) -2-(3-CF₃-pyridyl) CH N —CH₂CF₃ M291 (a and b) -2-(3-CHF₂-pyridyl) CHN —CH₂CF₃ M292 (a and b) -2-(3-hydroxypyridyl) CH N —CH₂CF₃ M293 (a andb) -2-(3-nitropyridyl) CH N —CH₂CF₃ M294 (a and b) -2-(3-cyanopyridyl)CH N —CH₂CF₃ M295 (a and b) -2-(3-bromopyridyl) CH N —CH₂CF₃ M296 (a andb) -2-(3-iodopyridyl) CH N —CH₂CF₃ M297 (a and b)-4-(5-chloropyrimidinyl) CH N —CH₂CF₃ M298 (a and b)-4-(5-methylpyrimidinyl) CH N —CH₂CF₃ M299 (a and b)-4-(5-fluoropyrimidinyl) CH N —CH₂CF₃ M300 (a and b)-2-(3-chloropyrazinyl) CH N —CH₂CF₃ M301 (a and b)-2-(3-methylpyrazinyl) CH N —CH₂CF₃ M302 (a and b)-2-(3-fluoropyrazinyl) CH N —CH₂CF₃ M303 (a and b)-3-(4-chloropyridazinyl) CH N —CH₂CF₃ M304 (a and b)-3-(4-methylpyridazinyl) CH N —CH₂CF₃ M305 (a and b)-3-(4-fluoropyridazinyl) CH N —CH₂CF₃ M306 (a and b)-5-(4-chlorothiadiazolyl) CH N —CH₂CF₃ M307 (a and b)-5-(4-methylthiadiazolyl) N N —CH₂CF₃ M308 (a and b)-5-(4-fluorothiadiazolyl) CH N —CH₂CF₃ M309 (a and b)-2-(3-chloropyridyl) N CH —OCF₃ M310 (a and b) -2-(3-fluoropyridyl) N CH—OCF₃ M311 (a and b) -2-(3-methylpyridyl) N CH —OCF₃ M312 (a and b)-2-(3-CF₃-pyridyl) N CH —OCF₃ M313 (a and b) -2-(3-CHF₂-pyridyl) N CH—OCF₃ M314 (a and b) -2-(3-hydroxypyridyl) N CH —OCF₃ M315 (a and b)-2-(3-nitropyridyl) N CH —OCF₃ M316 (a and b) -2-(3-cyanopyridyl) N CH—OCF₃ M317 (a and b) -2-(3-bromopyridyl) N CH —OCF₃ M318 (a and b)-2-(3-iodopyridyl) N CH —OCF₃ M319 (a and b) -4-(5-chloropyrimidinyl) NCH —OCF₃ M320 (a and b) -4-(5-methylpyrimidinyl) N CH —OCF₃ M321 (a andb) -4-(5-fluoropyrimidinyl) N CH —OCF₃ M322 (a and b)-2-(3-chloropyrazinyl) N CH —OCF₃ M323 (a and b) -2-(3-methylpyrazinyl)N CH —OCF₃ M324 (a and b) -2-(3-fluoropyrazinyl) N CH —OCF₃ M325 (a andb) -3-(4-chloropyridazinyl) N CH —OCF₃ M326 (a and b)-3-(4-methylpyridazinyl) N CH —OCF₃ M327 (a and b)-3-(4-fluoropyridazinyl) N CH —OCF₃ M328 (a and b)-5-(4-chlorothiadiazolyl) N CH —OCF₃ M329 (a and b)-5-(4-methylthiadiazolyl) N N —OCF₃ M330 (a and b)-5-(4-fluorothiadiazolyl) N CH —OCF₃ M331 (a and b) -2-(3-chloropyridyl)CH N —OCF₃ M332 (a and b) -2-(3-fluoropyridyl) CH N —OCF₃ M333 (a and b)-2-(3-methylpyridyl) CH N —OCF₃ M334 (a and b) -2-(3-CF₃-pyridyl) CH N—OCF₃ M335 (a and b) -2-(3-CHF₂-pyridyl) CH N —OCF₃ M336 (a and b)-2-(3-hydroxypyridyl) CH N —OCF₃ M337 (a and b) -2-(3-nitropyridyl) CH N—OCF₃ M338 (a and b) -2-(3-cyanopyridyl) CH N —OCF₃ M339 (a and b)-2-(3-bromopyridyl) CH N —OCF₃ M340 (a and b) -2-(3-iodopyridyl) CH N—OCF₃ M341 (a and b) -4-(5-chloropyrimidinyl) CH N —OCF₃ M342 (a and b)-4-(5-methylpyrimidinyl) CH N —OCF₃ M343 (a and b)-4-(5-fluoropyrimidinyl) CH N —OCF₃ M344 (a and b)-2-(3-chloropyrazinyl) CH N —OCF₃ M345 (a and b) -2-(3-methylpyrazinyl)CH N —OCF₃ M346 (a and b) -2-(3-fluoropyrazinyl) CH N —OCF₃ M347 (a andb) -3-(4-chloropyridazinyl) CH N —OCF₃ M348 (a and b)-3-(4-methylpyridazinyl) CH N —OCF₃ M349 (a and b)-3-(4-fluoropyridazinyl) CH N —OCF₃ M350 (a and b)-5-(4-chlorothiadiazolyl) CH N —OCF₃ M351 (a and b)-5-(4-methylthiadiazolyl) N N —OCF₃ M352 (a and b)-5-(4-fluorothiadiazolyl) CH N —OCF₃ M353 (a and b) -2-(3-chloropyridyl)N CH —SCF₃ M354 (a and b) -2-(3-fluoropyridyl) N CH —SCF₃ M355 (a and b)-2-(3-methylpyridyl) N CH —SCF₃ M356 (a and b) -2-(3-CF₃-pyridyl) N CH—SCF₃ M357 (a and b) -2-(3-CHF₂-pyridyl) N CH —SCF₃ M358 (a and b)-2-(3-hydroxypyridyl) N CH —SCF₃ M359 (a and b) -2-(3-nitropyridyl) N CH—SCF₃ M360 (a and b) -2-(3-cyanopyridyl) N CH —SCF₃ M361 (a and b)-2-(3-bromopyridyl) N CH —SCF₃ M362 (a and b) -2-(3-iodopyridyl) N CH—SCF₃ M363 (a and b) -4-(5-chloropyrimidinyl) N CH —SCF₃ M364 (a and b)-4-(5-methylpyrimidinyl) N CH —SCF₃ M365 (a and b)-4-(5-fluoropyrimidinyl) N CH —SCF₃ M366 (a and b)-2-(3-chloropyrazinyl) N CH —SCF₃ M367 (a and b) -2-(3-methylpyrazinyl)N CH —SCF₃ M368 (a and b) -2-(3-fluoropyrazinyl) N CH —SCF₃ M369 (a andb) -3-(4-chloropyridazinyl) N CH —SCF₃ M370 (a and b)-3-(4-methylpyridazinyl) N CH —SCF₃ M371 (a and b)-3-(4-fluoropyridazinyl) N CH —SCF₃ M372 (a and b)-5-(4-chlorothiadiazolyl) N CH —SCF₃ M373 (a and b)-5-(4-methylthiadiazolyl) N N —SCF₃ M374 (a and b)-5-(4-fluorothiadiazolyl) N CH —SCF₃ M375 (a and b) -2-(3-chloropyridyl)CH N —SCF₃ M376 (a and b) -2-(3-fluoropyridyl) CH N —SCF₃ M377 (a and b)-2-(3-methylpyridyl) CH N —SCF₃ M378 (a and b) -2-(3-CF₃-pyridyl) CH N—SCF₃ M379 (a and b) -2-(3-CHF₂-pyridyl) CH N —SCF₃ M380 (a and b)-2-(3-hydroxypyridyl) CH N —SCF₃ M381 (a and b) -2-(3-nitropyridyl) CH N—SCF₃ M382 (a and b) -2-(3-cyanopyridyl) CH N —SCF₃ M383 (a and b)-2-(3-bromopyridyl) CH N —SCF₃ M384 (a and b) -2-(3-iodopyridyl) CH N—SCF₃ M385 (a and b) -4-(5-chloropyrimidinyl) CH N —SCF₃ M386 (a and b)-4-(5-methylpyrimidinyl) CH N —SCF₃ M387 (a and b)-4-(5-fluoropyrimidinyl) CH N —SCF₃ M388 (a and b)-2-(3-chloropyrazinyl) CH N —SCF₃ M389 (a and b) -2-(3-methylpyrazinyl)CH N —SCF₃ M390 (a and b) -2-(3-fluoropyrazinyl) CH N —SCF₃ M391 (a andb) -3-(4-chloropyridazinyl) CH N —SCF₃ M392 (a and b)-3-(4-methylpyridazinyl) CH N —SCF₃ M393 (a and b)-3-(4-fluoropyridazinyl) CH N —SCF₃ M394 (a and b)-5-(4-chlorothiadiazolyl) CH N —SCF₃ M395 (a and b)-5-(4-methylthiadiazolyl) N N —SCF₃ M396 (a and b)-5-(4-fluorothiadiazolyl) CH N —SCF₃ M397 (a and b) -2-(3-chloropyridyl)N CH —H M398 (a and b) -2-(3-fluoropyridyl) N CH —H M399 (a and b)-2-(3-methylpyridyl) N CH —H M400 (a and b) -2-(3-CF₃-pyridyl) N CH —HM401 (a and b) -2-(3-CHF₂-pyridyl) N CH —H M402 (a and b)-2-(3-hydroxypyridyl) N CH —H M403 (a and b) -2-(3-nitropyridyl) N ClI—H M404 (a and b) -2-(3-cyanopyridyl) N CH —H M405 (a and b)-2-(3-bromopyridyl) N CH —H M406 (a and b) -2-(3-iodopyridyl) N CH —HM407 (a and b) -4-(5-chloropyrimidinyl) N CH —H M408 (a and b)-4-(5-methylpyrimidinyl) N CH —H M409 (a and b) -4-(5-fluoropyrimidinyl)N CH —H M410 (a and b) -2-(3-chloropyrazinyl) N CH —H M411 (a and b)-2-(3-methylpyrazinyl) N CH —H M412 (a and b) -2-(3-fluoropyrazinyl) NCH —H M413 (a and b) -3-(4-chloropyridazinyl) N CH —H M414 (a and b)-3-(4-methylpyridazinyl) N CH —H M415 (a and b) -3-(4-fluoropyridazinyl)N CH —H M416 (a and b) -5-(4-chlorothiadiazolyl) N CH —H M417 (a and b)-5-(4-methylthiadiazolyl) N N —H M418 (a and b)-5-(4-fluorothiadiazolyl) N CH —H M419 (a and b) -2-(3-chloropyridyl) CHN —H M420 (a and b) -2-(3-fluoropyridyl) CH N —H M421 (a and b)-2-(3-methylpyridyl) CH N —H M422 (a and b) -2-(3-CF₃-pyridyl) CH N —HM423 (a and b) -2-(3-CHF₂-pyridyl) CH N —H M424 (a and b)-2-(3-hydroxypyridyl) CH N —H M425 (a and b) -2-(3-nitropyridyl) CH N —HM426 (a and b) -2-(3-cyanopyridyl) CH N —H M427 (a and b)-2-(3-bromopyridyl) CH N —H M428 (a and b) -2-(3-iodopyridyl) CH N —HM429 (a and b) -4-(5-chloropyrimidinyl) CH N —H M430 (a and b)-4-(5-methylpyrimidinyl) CH N —H M431 (a and b) -4-(5-fluoropyrimidinyl)CH N —H M432 (a and b) -2-(3-chloropyrazinyl) CH N —H M433 (a and b)-2-(3-methylpyrazinyl) CH N —H M434 (a and b) -2-(3-fluoropyrazinyl) CHN —H M435 (a and b) -3-(4-chloropyridazinyl) CH N —H M436 (a and b)-3-(4-methylpyridazinyl) CH N —H M437 (a and b) -3-(4-fluoropyridazinyl)CH N —H M438 (a and b) -5-(4-chlorothiadiazolyl) CH N —H M439 (a and b)-5-(4-methylthiadiazolyl) N N —H M440 (a and b)-5-(4-fluorothiadiazolyl) CH N —H (a) means that R₃ is —H. (b) meansthat R₃ is —CH₃.

TABLE 14 (In)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  N1 (a and b) —H —H  N2 (a and b) —H -tert-butyl  N3 (a and b) —H-iso-butyl  N4 (a and b) —H -sec-butyl  N5 (a and b) —H -iso-propyl  N6(a and b) —H -n-propyl  N7 (a and b) —H -cyclohexyl  N8 (a and b) —H-tert-butoxy  N9 (a and b) —H -isopropoxy  N10 (a and b) —H —CF₃  N11 (aand b) —H —CH₂CF₃  N12 (a and b) —H —OCF₃  N13 (a and b) —H —Cl  N14 (aand b) —H —Br  N15 (a and b) —H —I  N16 (a and b) —H -n-butyl  N17 (aand b) —H —CH₃  N18 (a and b) —H —SCF₃  N19 (a and b) —H —N(CH₂CH₃)₂ N20 (a and b) —H —OCF₂CHF₂  N21 (a and b) —H —C(OH)(CF₃)₂  N22 (a andb) —H -(1,1-dimethyl-pentyl)  N23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester  N24 (a and b) —H —N-piperidinyl  N25 (a and b) —Cl —H N26 (a and b) —Cl -tert-butyl  N27 (a and b) —Cl -iso-butyl  N28 (a andb) —Cl -sec-butyl  N29 (a and b) —Cl -iso-propyl  N30 (a and b) —Cl-n-propyl  N31 (a and b) —Cl -cyclohexyl  N32 (a and b) —Cl -tert-butoxy N33 (a and b) —Cl -isopropoxy  N34 (a and b) —Cl —CF₃  N35 (a and b)—Cl —CH₂CF₃  N36 (a and b) —Cl —OCF₃  N37 (a and b) —Cl —Cl  N38 (a andb) —Cl —Br  N39 (a and b) —Cl —I  N40 (a and b) —Cl -n-butyl  N41 (a andb) —Cl —CH₃  N42 (a and b) —Cl —SCF₃  N43 (a and b) —Cl —N(CH₂CH₃)₂  N44(a and b) —Cl —OCF₂CHF₂  N45 (a and b) —Cl —C(OH)(CF₃)₂  N46 (a and b)—Cl -(1,1-dimethyl-pentyl)  N47 (a and b) —Cl -(1,1-dimethyl-aceticacid) ethyl ester  N48 (a and b) —Cl —N-piperidinyl  N49 (a and b) —F —H N50 (a and b) —F -tert-butyl  N51 (a and b) —F -iso-butyl  N52 (a andb) —F -sec-butyl  N53 (a and b) —F -iso-propyl  N54 (a and b) —F-n-propyl  N55 (a and b) —F -cyclohexyl  N56 (a and b) —F -tert-butoxy N57 (a and b) —F -isopropoxy  N58 (a and b) —F —CF₃  N59 (a and b) —F—CH₂CF₃  N60 (a and b) —F —OCF₃  N61 (a and b) —F —Cl  N62 (a and b) —F—Br  N63 (a and b) —F —I  N64 (a and b) —F -n-butyl  N65 (a and b) —F—CH₃  N66 (a and b) —F —SCF₃  N67 (a and b) —F —N(CH₂CH₃)₂  N68 (a andb) —F —OCF₂CHF₂  N69 (a and b) —F —C(OH)(CF₃)₂  N70 (a and b) —F-(1,1-dimethyl-pentyl)  N71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester  N72 (a and b) —F —N-piperidinyl  N73 (a and b) —CH₃ —H  N74(a and b) —CH₃ -iso-butyl  N75 (a and b) —CH₃ -tert-butyl  N76 (a and b)—CH₃ -sec-butyl  N77 (a and b) —CH₃ -iso-propyl  N78 (a and b) —CH₃-n-propyl  N79 (a and b) —CH₃ -cyclohexyl  N80 (a and b) —CH₃-tert-butoxy  N81 (a and b) —CH₃ -isopropoxy  N82 (a and b) —CH₃ —CF₃ N83 (a and b) —CH₃ —CH₂CF₃  N84 (a and b) —CH₃ —OCF₃  N85 (a and b)—CH₃ —Cl  N86 (a and b) —CH₃ —Br  N87 (a and b) —CH₃ —I  N88 (a and b)—CH₃ -n-butyl  N89 (a and b) —CH₃ —CH₃  N90 (a and b) —CH₃ —SCF₃  N91 (aand b) —CH₃ —N(CH₂CH₃)₂  N92 (a and b) —CH₃ —OCF₂CHF₂  N93 (a and b)—CH₃ —C(OH)(CF₃)₂  N94 (a and b) —CH₃ -(1,1-dimethyl-pentyl)  N95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester  N96 (a and b) —CH₃—N-piperidinyl  N97 (a and b) —CF₃ —H  N98 (a and b) —CF₃ -tert-butyl N99 (a and b) —CF₃ -iso-butyl N100 (a and b) —CF₃ -sec-butyl N101 (aand b) —CF₃ -iso-propyl N102 (a and b) —CF₃ -n-propyl N103 (a and b)—CF₃ -cyclohexyl N104 (a and b) —CF₃ -tert-butoxy N105 (a and b) —CF₃-isopropoxy N106 (a and b) —CF₃ —CF₃ N107 (a and b) —CF₃ —CH₂CF₃ N108 (aand b) —CF₃ —OCF₃ N109 (a and b) —CF₃ —Cl N110 (a and b) —CF₃ —Br N111(a and b) —CF₃ —I N112 (a and b) —CF₃ -n-butyl N113 (a and b) —CF₃ —CH₃N114 (a and b) —CF₃ —SCF₃ N115 (a and b) —CF₃ —N(CH₂CH₃)₂ N116 (a and b)—CF₃ —OCF₂CHF₂ N117 (a and b) —CF₃ —C(OH)(CF₃)₂ N118 (a and b) —CF₃-(1,1-dimethyl-pentyl) N119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester N120 (a and b) —CF₃ —N-piperidinyl N121 (a and b) —CHF₂-tert-butyl N122 (a and b) —CHF₂ —H N123 (a and b) —CHF₂ -iso-butyl N124(a and b) —CHF₂ -sec-butyl N125 (a and b) —CHF₂ -iso-propyl N126 (a andb) —CHF₂ -n-propyl N127 (a and b) —CHF₂ -cyclohexyl N128 (a and b) —CHF₂-tert-butoxy N129 (a and b) —CHF₂ -isopropoxy N130 (a and b) —CHF₂ —CF₃N131 (a and b) —CHF₂ —CH₂CF₃ N132 (a and b) —CHF₂ —OCF₃ N133 (a and b)—CHF₂ —Cl N134 (a and b) —CHF₂ —Br N135 (a and b) —CHF₂ —I N136 (a andb) —CHF₂ -n-butyl N137 (a and b) —CHF₂ —CH₃ N138 (a and b) —CHF₂ —SCF₃N139 (a and b) —CHF₂ —N(CH₂CH₃)₂ N140 (a and b) —CHF₂ —OCF₂CHF₂ N141 (aand b) —CHF₂ —C(OH)(CF₃)₂ N142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)N143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester N144 (a andb) —CHF₂ —N-piperidinyl N145 (a and b) —OH —H N146 (a and b) —OH-tert-butyl N147 (a and b) —OH -iso-butyl N148 (a and b) —OH -sec-butylN149 (a and b) —OH -iso-propyl N150 (a and b) —OH -n-propyl N151 (a andb) —OH -cyclohexyl N152 (a and b) —OH -tert-butoxy N153 (a and b) —OH-isopropoxy N154 (a and b) —OH —CF₃ N155 (a and b) —OH —CH₂CF₃ N156 (aand b) —OH —OCF₃ N157 (a and b) —OH —Cl N158 (a and b) —OH —Br N159 (aand b) —OH —I N160 (a and b) —OH -n-butyl N161 (a and b) —OH —CH₃ N162(a and b) —OH —SCF₃ N163 (a and b) —OH —N(CH₂CH₃)₂ N164 (a and b) —OH—OCF₂CHF₂ N165 (a and b) —OH —C(OH)(CF₃)₂ N166 (a and b) —OH-(1,1-dimethyl-pentyl) N167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester N168 (a and b) —OH —N-piperidinyl N169 (a and b) —NO₂ —HN170 (a and b) —NO₂ -tert-butyl N171 (a and b) —NO₂ -iso-butyl N172 (aand b) —NO₂ -sec-butyl N173 (a and b) —NO₂ -iso-propyl N174 (a and b)—NO₂ -n-propyl N175 (a and b) —NO₂ -cyclohexyl N176 (a and b) —NO₂-tert-butoxy N177 (a and b) —NO₂ -isopropoxy N178 (a and b) —NO₂ —CF₃N179 (a and b) —NO₂ —CH₂CF₃ N180 (a and b) —NO₂ —OCF₃ N181 (a and b)—NO₂ —Cl N182 (a and b) —NO₂ —Br N183 (a and b) —NO₂ —I N184 (a and b)—NO₂ -n-butyl N185 (a and b) —NO₂ —CH₃ N186 (a and b) —NO₂ —SCF₃ N187 (aand b) —NO₂ —N(CH₂CH₃)₂ N188 (a and b) —NO₂ —OCF₂CHF₂ N189 (a and b)—NO₂ —C(OH)(CF₃)₂ N190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) N191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester N192 (a and b) —NO₂—N-piperidinyl N193 (a and b) —CN —H N194 (a and b) —CN -tert-butyl N195(a and b) —CN -iso-butyl N196 (a and b) —CN -sec-butyl N197 (a and b)—CN -iso-propyl N198 (a and b) —CN -n-propyl N199 (a and b) —CN-cyclohexyl N200 (a and b) —CN -tert-butoxy N201 (a and b) —CN-isopropoxy N202 (a and b) —CN —CF₃ N203 (a and b) —CN —CH₂CF₃ N204 (aand b) —CN —OCF₃ N205 (a and b) —CN —Cl N206 (a and b) —CN —Br N207 (aand b) —CN —I N208 (a and b) —CN -n-butyl N209 (a and b) —CN —CH₃ N210(a and b) —CN —SCF₃ N211 (a and b) —CN —N(CH₂CH₃)₂ N212 (a and b) —CN—OCF₂CHF₂ N213 (a and b) —CN —C(OH)(CF₃)₂ N214 (a and b) —CN-(1,1-dimethyl-pentyl) N215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester N216 (a and b) —CN —N-piperidinyl N217 (a and b) —Br —H N218(a and b) —Br -tert-butyl N219 (a and b) —Br -iso-butyl N220 (a and b)—Br -sec-butyl N221 (a and b) —Br -iso-propyl N222 (a and b) —Br-n-propyl N223 (a and b) —Br -cyclohexyl N224 (a and b) —Br -tert-butoxyN225 (a and b) —Br -isopropoxy N226 (a and b) —Br —CF₃ N227 (a and b)—Br —CH₂CF₃ N228 (a and b) —Br —OCF₃ N229 (a and b) —Br —Cl N230 (a andb) —Br —Br N231 (a and b) —Br —I N232 (a and b) —Br -n-butyl N233 (a andb) —Br —CH₃ N234 (a and b) —Br —SCF₃ N235 (a and b) —Br —N(CH₂CH₃)₂ N236(a and b) —Br —OCF₂CHF₂ N237 (a and b) —Br —C(OH)(CF₃)₂ N238 (a and b)—Br -(1,1-dimethyl-pentyl) N239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester N240 (a and b) —Br —N-piperidinyl N241 (a and b) —I-tert-butyl N242 (a and b) —I —H N243 (a and b) —I -iso-butyl N244 (aand b) —I -sec-butyl N245 (a and b) —I -iso-propyl N246 (a and b) —I-n-propyl N247 (a and b) —I -cyclohexyl N248 (a and b) —I -tert-butoxyN249 (a and b) —I -isopropoxy N250 (a and b) —I —CF₃ N251 (a and b) —I—CH₂CF₃ N252 (a and b) —I —OCF₃ N253 (a and b) —I —Cl N254 (a and b) —I—Br N255 (a and b) —I —I N256 (a and b) —I -n-butyl N257 (a and b) —I—CH₃ N258 (a and b) —I —SCF₃ N259 (a and b) —I —N(CH₂CH₃)₂ N260 (a andb) —I —OCF₂CHF₂ N261 (a and b) —I —C(OH)(CF₃)₂ N262 (a and b) —I-(1,1-dimethyl-pentyl) N263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester N264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 15 (Io)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a) O1 (a and b) —H —H O2 (a and b) —H -tert-butyl O3 (a and b) —H-iso-butyl O4 (a and b) —H -sec-butyl O5 (a and b) —H -iso-propyl O6 (aand b) —H -n-propyl O7 (a and b) —H -cyclohexyl O8 (a and b) —H-tert-butoxy O9 (a and b) —H -isopropoxy O10 (a and b) —H —CF₃ O11 (aand b) —H —CH₂CF₃ O12 (a and b) —H —OCF₃ O13 (a and b) —H —Cl O14 (a andb) —H —Br O15 (a and b) —H —I O16 (a and b) —H -n-butyl O17 (a and b) —H—CH₃ O18 (a and b) —H —SCF₃ O19 (a and b) —H —N(CH₂CH₃)₂ O20 (a and b)—H —OCF₂CHF₂ O21 (a and b) —H —C(OH)(CF₃)₂ O22 (a and b) —H-(1,1-dimethyl-pentyl) O23 (a and b) —H -(1,1-dimethyl-acetic acid)ethyl ester O24 (a and b) —H —N-piperidinyl O25 (a and b) —Cl —H O26 (aand b) —Cl -tert-butyl O27 (a and b) —Cl -iso-butyl O28 (a and b) —Cl-sec-butyl O29 (a and b) —Cl -iso-propyl O30 (a and b) —Cl -n-propyl O31(a and b) —Cl -cyclohexyl O32 (a and b) —Cl -tert-butoxy O33 (a and b)—Cl -isopropoxy O34 (a and b) —Cl —CF₃ O35 (a and b) —Cl —CH₂CF₃ O36 (aand b) —Cl —OCF₃ O37 (a and b) —Cl —Cl O38 (a and b) —Cl —Br O39 (a andb) —Cl —I O40 (a and b) —Cl -n-butyl O41 (a and b) —Cl —CH₃ O42 (a andb) —Cl —SCF₃ O43 (a and b) —Cl —N(CH₂CH₃)₂ O44 (a and b) —Cl —OCF₂CHF₂O45 (a and b) —Cl —C(OH)(CF₃)₂ O46 (a and b) —Cl -(1,1-dimethyl-pentyl)O47 (a and b) —Cl -(1,1-dimethyl-acetic acid) ethyl ester O48 (a and b)—Cl —N-piperidinyl O49 (a and b) —F —H O50 (a and b) —F -tert-butyl O51(a and b) —F -iso-butyl O52 (a and b) —F -sec-butyl O53 (a and b) —F-iso-propyl O54 (a and b) —F -n-propyl O55 (a and b) —F -cyclohexyl O56(a and b) —F -tert-butoxy O57 (a and b) —F -isopropoxy O58 (a and b) —F—CF₃ O59 (a and b) —F —CH₂CF₃ O60 (a and b) —F —OCF₃ O61 (a and b) —F—Cl O62 (a and b) —F —Br O63 (a and b) —F —I O64 (a and b) —F -n-butylO65 (a and b) —F —CH₃ O66 (a and b) —F —SCF₃ O67 (a and b) —F—N(CH₂CH₃)₂ O68 (a and b) —F —OCF₂CHF₂ O69 (a and b) —F —C(OH)(CF₃)₂ O70(a and b) —F -(1,1-dimethyl-pentyl) O71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester O72 (a and b) —F —N-piperidinylO73 (a and b) —CH₃ —H O74 (a and b) —CH₃ -tert-butyl O75 (a and b) —CH₃-iso-butyl O76 (a and b) —CH₃ -sec-butyl O77 (a and b) —CH₃ -iso-propylO78 (a and b) —CH₃ -n-propyl O79 (a and b) —CH₃ -cyclohexyl O80 (a andb) —CH₃ -tert-butoxy O81 (a and b) —CH₃ -isopropoxy O82 (a and b) —CH₃—CF₃ O83 (a and b) —CH₃ —CH₂CF₃ O84 (a and b) —CH₃ —OCF₃ O85 (a and b)—CH₃ —Cl O86 (a and b) —CH₃ —Br O87 (a and b) —CH₃ —I O88 (a and b) —CH₃-n-butyl O89 (a and b) —CH₃ —CH₃ O90 (a and b) —CH₃ —SCF₃ O91 (a and b)—CH₃ —N(CH₂CH₃)₂ O92 (a and b) —CH₃ —OCF₂CHF₂ O93 (a and b) —CH₃—C(OH)(CF₃)₂ O94 (a and b) —CH₃ -(1,1-dimethyl-pentyl) O95 (a and b)—CH₃ -(1,1-dimethyl-acetic acid) ethyl ester O96 (a and b) —CH₃—N-piperidinyl O97 (a and b) —CF₃ —H O98 (a and b) —CF₃ -tert-butyl O99(a and b) —CF₃ -iso-butyl O100 (a and b) —CF₃ -sec-butyl O101 (a and b)—CF₃ -iso-propyl O102 (a and b) —CF₃ -n-propyl O103 (a and b) —CF₃-cyclohexyl O104 (a and b) —CF₃ -tert-butoxy O105 (a and b) —CF₃-isopropoxy O106 (a and b) —CF₃ —CF₃ O107 (a and b) —CF₃ —CH₂CF₃ O108 (aand b) —CF₃ —OCF₃ O109 (a and b) —CF₃ —Cl O110 (a and b) —CF₃ —Br O111(a and b) —CF₃ —I O112 (a and b) —CF₃ -n-butyl O113 (a and b) —CF₃ —CH₃O114 (a and b) —CF₃ —SCF₃ O115 (a and b) —CF₃ —N(CH₂CH₃)₂ O116 (a and b)—CF₃ —OCF₂CHF₂ O117 (a and b) —CF₃ —C(OH)(CF₃)₂ O118 (a and b) —CF₃-(1,1-dimethyl-pentyl) O119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester O120 (a and b) —CF₃ —N-piperidinyl O121 (a and b) —CHF₂-tert-butyl O122 (a and b) —CHF₂ —H O123 (a and b) —CHF₂ -iso-butyl O124(a and b) —CHF₂ -sec-butyl O125 (a and b) —CHF₂ -iso-propyl O126 (a andb) —CHF₂ -n-propyl O127 (a and b) —CHF₂ -cyclohexyl O128 (a and b) —CHF₂-tert-butoxy O129 (a and b) —CHF₂ -isopropoxy O130 (a and b) —CHF₂ —CF₃O131 (a and b) —CHF₂ —CH₂CF₃ O132 (a and b) —CHF₂ —OCF₃ O133 (a and b)—CHF₂ —Cl O134 (a and b) —CHF₂ —Br O135 (a and b) —CHF₂ —I O136 (a andb) —CHF₂ -n-butyl O137 (a and b) —CHF₂ —CH₃ O138 (a and b) —CHF₂ —SCF₃O139 (a and b) —CHF₂ —N(CH₂CH₃)₂ O140 (a and b) —CHF₂ —O_(—) O141 (a andb) —CHF₂ —C(OH)(CF₃)₂ O142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl) O143(a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester O144 (a and b)—CHF₂ —N-piperidinyl O145 (a and b) —OH —H O146 (a and b) —OH-tert-butyl O147 (a and b) —OH -iso-butyl O148 (a and b) —OH -sec-butylO149 (a and b) —OH -iso-propyl O150 (a and b) —OH -n-propyl O151 (a andb) —OH -cyclohexyl O152 (a and b) —OH -tert-butoxy O153 (a and b) —OH-isopropoxy O154 (a and b) —OH —CF₃ O155 (a and b) —OH —CH₂CF₃ O156 (aand b) —OH —OCF₃ O157 (a and b) —OH —Cl O158 (a and b) —OH —Br O159 (aand b) —OH —I O160 (a and b) —OH -n-butyl O161 (a and b) —OH —CH₃ O162(a and b) —OH —SCF₃ O163 (a and b) —OH —N(CH₂CH₃)₂ O164 (a and b) —OH—OCF₂CHF₂ O165 (a and b) —OH —C(OH)(CF₃)₂ O166 (a and b) —OH-(1,1-dimethyl-pentyl) O167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester O168 (a and b) —OH —N-piperidinyl O169 (a and b) —NO₂ —HO170 (a and b) —NO₂ -tert-butyl O171 (a and b) —NO₂ -iso-butyl O172 (aand b) —NO₂ -sec-butyl O173 (a and b) —NO₂ -iso-propyl O174 (a and b)—NO₂ -n-propyl O175 (a and b) —NO₂ -cyclohexyl O176 (a and b) —NO₂-tert-butoxy O177 (a and b) —NO₂ -isopropoxy O178 (a and b) —NO₂ —CF₃O179 (a and b) —NO₂ —CH₂CF₃ O180 (a and b) —NO₂ —OCF₃ O181 (a and b)—NO₂ —Cl O182 (a and b) —NO₂ —Br O183 (a and b) —NO₂ —I O184 (a and b)—NO₂ -n-butyl O185 (a and b) —NO₂ —CH₃ O186 (a and b) —NO₂ —SCF₃ O187 (aand b) —NO₂ —N(CH₂CH₃)₂ O188 (a and b) —NO₂ —OCF₂CHF₂ O189 (a and b)—NO₂ —C(OH)(CF₃)₂ O190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) O191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester O192 (a and b) —NO₂—N-piperidinyl O193 (a and b) —CN —H O194 (a and b) —CN -tert-butyl O195(a and b) —CN -iso-butyl O196 (a and b) —CN -sec-butyl O197 (a and b)—CN -iso-propyl O198 (a and b) —CN -n-propyl O199 (a and b) —CN-cyclohexyl O200 (a and b) —CN -tert-butoxy O201 (a and b) —CN-isopropoxy O202 (a and b) —CN —CF₃ O203 (a and b) —CN —CH₂CF₃ O204 (aand b) —CN —OCF₃ O205 (a and b) —CN —Cl O206 (a and b) —CN —Br O207 (aand b) —CN —I O208 (a and b) —CN -n-butyl O209 (a and b) —CN —CH₃ O210(a and b) —CN —SCF₃ O211 (a and b) —CN —N(CH₂CH₃)₂ O212 (a and b) —CN—OCF₂CHF₂ O213 (a and b) —CN —C(OH)(CF₃)₂ O214 (a and b) —CN-(1,1-dimethyl-pentyl) O215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester O216 (a and b) —CN —N-piperidinyl O217 (a and b) —Br —H O218(a and b) —Br -tert-butyl O219 (a and b) —Br -iso-butyl O220 (a and b)—Br -sec-butyl O221 (a and b) —Br -iso-propyl O222 (a and b) —Br-n-propyl O223 (a and b) —Br -cyclohexyl O224 (a and b) —Br -tert-butoxyO225 (a and b) —Br -isopropoxy O226 (a and b) —Br —CF₃ O227 (a and b)—Br —CH₂CF₃ O228 (a and b) —Br —OCF₃ O229 (a and b) —Br —Cl O230 (a andb) —Br —Br O231 (a and b) —Br —I O232 (a and b) —Br -n-butyl O233 (a andb) —Br —CH₃ O234 (a and b) —Br —SCF₃ O235 (a and b) —Br —N(CH₂CH₃)₂ O236(a and b) —Br —OCF₂CHF₂ O237 (a and b) —Br —C(OH)(CF₃)₂ O238 (a and b)—Br -(1,1-dimethyl-pentyl) O239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester O240 (a and b) —Br —N-piperidinyl O241 (a and b) —I-tert-butyl O242 (a and b) —I —H O243 (a and b) —I -iso-butyl O244 (aand b) —I -sec-butyl O245 (a and b) —I -iso-propyl O246 (a and b) —I-n-propyl O247 (a and b) —I -cyclohexyl O248 (a and b) —I -tert-butoxyO249 (a and b) —I -isopropoxy O250 (a and b) —I —CF₃ O251 (a and b) —I—CH₂CF₃ O252 (a and b) —I —OCF₃ O253 (a and b) —I —Cl O254 (a and b) —I—Br O255 (a and b) —I —I O256 (a and b) —I -n-butyl O257 (a and b) —I—CH₃ O258 (a and b) —I —SCF₃ O259 (a and b) —I —N(CH₂CH₃)₂ O260 (a andb) —I —OCF₂CHF₂ O261 (a and b) —I —C(OH)(CF₃)₂ O262 (a and b) —I-(1,1-dimethyl-pentyl) O263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester O264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 16 (Ip)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a) P1 (a and b) —H —H P2 (a and b) —H -tert-butyl P3 (a and b) —H-iso-butyl P4 (a and b) —H -sec-butyl P5 (a and b) —H -iso-propyl P6 (aand b) —H -n-propyl P7 (a and b) —H -cyclohexyl P8 (a and b) —H-tert-butoxy P9 (a and b) —H -isopropoxy P10 (a and b) —H —CF₃ P11 (aand b) —H —CH₂CF₃ P12 (a and b) —H —OCF₃ P13 (a and b) —H —Cl P14 (a andb) —H —Br P15 (a and b) —H —I P16 (a and b) —H -n-butyl P17 (a and b) —H—CH₃ P18 (a and b) —H —SCF₃ P19 (a and b) —H —N(CH₂CH₃)₂ P20 (a and b)—H —OCF₂CHF₂ P21 (a and b) —H —C(OH)(CF₃)₂ P22 (a and b) —H-(1,1-dimethyl-pentyl) P23 (a and b) —H -(1,1-dimethyl-acetic acid)ethyl ester P24 (a and b) —H —N-piperidinyl P25 (a and b) —Cl —H P26 (aand b) —Cl -tert-butyl P27 (a and b) —Cl -iso-butyl P28 (a and b) —Cl-sec-butyl P29 (a and b) —Cl -iso-propyl P30 (a and b) —Cl -n-propyl P31(a and b) —Cl -cyclohexyl P32 (a and b) —Cl -tert-butoxy P33 (a and b)—Cl -isopropoxy P34 (a and b) —Cl —CF₃ P35 (a and b) —Cl —CH₂CF₃ P36 (aand b) —Cl —OCF₃ P37 (a and b) —Cl —Cl P38 (a and b) —Cl —Br P39 (a andb) —Cl —I P40 (a and b) —Cl -n-butyl P41 (a and b) —Cl —CH₃ P42 (a andb) —Cl —SCF₃ P43 (a and b) —Cl —N(CH₂CH₃)₂ P44 (a and b) —Cl —OCF₂CHF₂P45 (a and b) —Cl —C(OH)(CF₃)₂ P46 (a and b) —Cl -(1,1-dimethyl-pentyl)P47 (a and b) —Cl -(1,1-dimethyl-acetic acid) ethyl ester P48 (a and b)—Cl —N-piperidinyl P49 (a and b) —F —H P50 (a and b) —F -tert-butyl P51(a and b) —F -iso-butyl P52 (a and b) —F -sec-butyl P53 (a and b) —F-iso-propyl P54 (a and b) —F -n-propyl P55 (a and b) —F -cyclohexyl P56(a and b) —F -tert-butoxy P57 (a and b) —F —is opropox y P58 (a and b)—F —CF₃ P59 (a and b) —F —CH₂CF₃ P60 (a and b) —F —OCF₃ P61 (a and b) —F—Cl P62 (a and b) —F —Br P63 (a and b) —F —I P64 (a and b) —F -n-butylP65 (a and b) —F —CH₃ P66 (a and b) —F —SCF₃ P67 (a and b) —F—N(CH₂CH₃)₂ P68 (a and b) —F —OCF₂CHF₂ P69 (a and b) —F —C(OH)(CF₃)₂ P70(a and b) —F -(1,1-dimethyl-pentyl) P71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester P72 (a and b) —F —N-piperidinylP73 (a and b) —CH₃ —H P74 (a and b) —CH₃ -iso-butyl P75 (a and b) —CH₃-tert-butyl P76 (a and b) —CH₃ -sec-butyl P77 (a and b) —CH₃ -iso-propylP78 (a and b) —CH₃ -n-propyl P79 (a and b) —CH₃ -cyclohexyl P80 (a andb) —CH₃ -tert-butoxy P81 (a and b) —CH₃ -isopropoxy P82 (a and b) —CH₃—CF₃ P83 (a and b) —CH₃ —CH₂CF₃ P84 (a and b) —CH₃ —OCF₃ P85 (a and b)—CH₃ —Cl P86 (a and b) —CH₃ —Br P87 (a and b) —CH₃ —I P88 (a and b) —CH₃-n-butyl P89 (a and b) —CH₃ —CH₃ P90 (a and b) —CH₃ —SCF₃ P91 (a and b)—CH₃ —N(CH₂CH₃)₂ P92 (a and b) —CH₃ —OCF₂CHF₂ P93 (a and b) —CH₃—C(OH)(CF₃)₂ P94 (a and b) —CH₃ -(1,1-dimethyl-pentyl) P95 (a and b)—CH₃ -(1,1-dimethyl-acetic acid) ethyl ester P96 (a and b) —CH₃—N-piperidinyl P97 (a and b) —CF₃ —H P98 (a and b) —CF₃ -tert-butyl P99(a and b) —CF₃ -iso-butyl P100 (a and b) —CF₃ -sec-butyl P101 (a and b)—CF₃ -iso-propyl P102 (a and b) —CF₃ -n-propyl P103 (a and b) —CF₃-cyclohexyl P104 (a and b) —CF₃ -tert-butoxy P105 (a and b) —CF₃-isopropoxy P106 (a and b) —CF₃ —CF₃ P107 (a and b) —CF₃ —CH₂CF₃ P108 (aand b) —CF₃ —OCF₃ P109 (a and b) —CF₃ —Cl P110 (a and b) —CF₃ —Br P111(a and b) —CF₃ —I P112 (a and b) —CF₃ -n-butyl P113 (a and b) —CF₃ —CH₃P114 (a and b) —CF₃ —SCF₃ P115 (a and b) —CF₃ —N(CH₂CH₃)₂ P116 (a and b)—CF₃ —OCF₂CHF₂ P117 (a and b) —CF₃ —C(OH)(CF₃)₂ P118 (a and b) —CF₃-(1,1-dimethyl-pentyl) P119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester P120 (a and b) —CF₃ —N-piperidinyl P121 (a and b) —CHF₂-tert-butyl P122 (a and b) —CHF₂ —H P123 (a and b) —CHF₂ -iso-butyl P124(a and b) —CHF₂ -sec-butyl P125 (a and b) —CHF₂ -iso-propyl P126 (a andb) —CHF₂ -n-propyl P127 (a and b) —CHF₂ -cyclohexyl P128 (a and b) —CHF₂-tert-butoxy P129 (a and b) —CHF₂ -isopropoxy P130 (a and b) —CHF₂ —CF₃P131 (a and b) —CHF₂ —CH₂CF₃ P132 (a and b) —CHF₂ —OCF₃ P133 (a and b)—CHF₂ —CI P134 (a and b) —CHF₂ —Br P135 (a and b) —CHF₂ —I P136 (a andb) —CHF₂ -n-butyl P137 (a and b) —CHF₂ —CH₃ P138 (a and b) —CHF₂ —SCF₃P139 (a and b) —CHF₂ —N(CH₂CH₃)₂ P140 (a and b) —CHF₂ —OCF₂CHF₂ P141 (aand b) —CHF₂ —C(OH)(CF₃)₂ P142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)P143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester P144 (a andb) —CHF₂ —N-piperidinyl P145 (a and b) —OH —H P146 (a and b) —OH-tert-butyl P147 (a and b) —OH -iso-butyl P148 (a and b) —OH -sec-butylP149 (a and b) —OH -iso-propyl P150 (a and b) —OH -n-propyl P151 (a andb) —OH -cyclohexyl P152 (a and b) —OH -tert-butoxy P153 (a and b) —OH-isopropoxy P154 (a and b) —OH —CF₃ P155 (a and b) —OH —CH₂CF₃ P156 (aand b) —OH —OCF₃ P157 (a and b) —OH —Cl P158 (a and b) —OH —Br P159 (aand b) —OH —I P160 (a and b) —OH -n-butyl P161 (a and b) —OH —CH₃ P162(a and b) —OH —SCF₃ P163 (a and b) —OH —N(CH₂CH₃)₂ P164 (a and b) —OH—OCF₂CHF₂ P165 (a and b) —OH —C(OH)(CF₃)₂ P166 (a and b) —OH-(1,1-dimethyl-pentyl) P167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester P168 (a and b) —OH —N-piperidinyl P169 (a and b) —NO₂ —HP170 (a and b) —NO₂ -tert-butyl P171 (a and b) —NO₂ -iso-butyl P172 (aand b) —NO₂ -sec-butyl P173 (a and b) —NO₂ -iso-propyl P174 (a and b)—NO₂ -n-propyl P175 (a and b) —NO₂ -cyclohexyl P176 (a and b) —NO₂-tert-butoxy P177 (a and b) —NO₂ -isopropoxy P178 (a and b) —NO₂ —CF₃P179 (a and b) —NO₂ —CH₂CF₃ P180 (a and b) —NO₂ —OCF₃ P181 (a and b)—NO₂ —Cl P182 (a and b) —NO₂ —Br P183 (a and b) —NO₂ —I P184 (a and b)—NO₂ -n-butyl P185 (a and b) —NO₂ —CH₃ P186 (a and b) —NO₂ —SCF₃ P187 (aand b) —NO₂ —N(CH₂CH₃)₂ P188 (a and b) —NO₂ —OCF₂CHF₂ P189 (a and b)—NO₂ —C(OH)(CF₃)₂ P190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) P191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester P192 (a and b) —NO₂—N-piperidinyl P193 (a and b) —CN —H P194 (a and b) —CN -tert-butyl P195(a and b) —CN -iso-butyl P196 (a and b) —CN -sec-butyl P197 (a and b)—CN -iso-propyl P198 (a and b) —CN -n-propyl P199 (a and b) —CN-cyclohexyl P200 (a and b) —CN -tert-butoxy P201 (a and b) —CN-isopropoxy P202 (a and b) —CN —CF₃ P203 (a and b) —CN —CH₂CF₃ P204 (aand b) —CN —OCF₃ P205 (a and b) —CN —Cl P206 (a and b) —CN —Br P207 (aand b) —CN —I P208 (a and b) —CN -n-butyl P209 (a and b) —CN —CH₃ P210(a and b) —CN —SCF₃ P211 (a and b) —CN —N(CH₂CH₃)₂ P212 (a and b) —CN—OCF₂CHF₂ P213 (a and b) —CN —C(OH)(CF₃)₂ P214 (a and b) —CN-(1,1-dimethyl-pentyl) P215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester P216 (a and b) —CN —N-piperidinyl P217 (a and b) —Br —H P218(a and b) —Br -tert-butyl P219 (a and b) —Br -iso-butyl P220 (a and b)—Br -sec-butyl P221 (a and b) —Br -iso-propyl P222 (a and b) —Br-n-propyl P223 (a and b) —Br -cyclohexyl P224 (a and b) —Br -tert-butoxyP225 (a and b) —Br -isopropoxy P226 (a and b) —Br —CF₃ P227 (a and b)—Br —CH₂CF₃ P228 (a and b) —Br —CH₂CF₃ P229 (a and b) —Br —Cl P230 (aand b) —Br —Br P231 (a and b) —Br —I P232 (a and b) —Br -n-butyl P233 (aand b) —Br —CH₃ P234 (a and b) —Br —SCF₃ P235 (a and b) —Br —N(CH₂CH₃)₂P236 (a and b) —Br —OCF₂CHF₂ P237 (a and b) —Br —C(OH)(CF₃)₂ P238 (a andb) —Br -(1,1-dimethyl-pentyl) P239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester P240 (a and b) —Br —N-piperidinyl P241 (a and b) —I-tert-butyl P242 (a and b) —I —H P243 (a and b) —I -iso-butyl P244 (aand b) —I -sec-butyl P245 (a and b) —I -iso-propyl P246 (a and b) —I-n-propyl P247 (a and b) —I -cyclohexyl P248 (a and b) —I -tert-butoxyP249 (a and b) —I -isopropoxy P250 (a and b) —I —CF₃ P251 (a and b) —I—CH₂CF₃ P252 (a and b) —I —OCF₃ P253 (a and b) —I —Cl P254 (a and b) —I—Br P255 (a and b) —I —I P256 (a and b) —I -n-butyl P257 (a and b) —I—CH₃ P258 (a and b) —I —SCF₃ P259 (a and b) —I —N(CH₂CH₃)₂ P260 (a andb) —I —OCF₂CHF₂ P261 (a and b) —I —C(OH)(CF₃)₂ P262 (a and b) —I-(1,1-dimethyl-pentyl) P263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester P264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 17 (Iq)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a) Q1 (a and b) —H —H Q2 (a and b) —H -tert-butyl Q3 (a and b) —H-iso-butyl Q4 (a and b) —H -sec-butyl Q5 (a and b) —H -iso-propyl Q6 (aand b) —H -n-propyl Q7 (a and b) —H -cyclohexyl Q8 (a and b) —H-tert-butoxy Q9 (a and b) —H -isopropoxy Q10 (a and b) —H —CF₃ Q11 (aand b) —H —CH₂CF₃ Q12 (a and b) —H —OCF₃ Q13 (a and b) —H —Cl Q14 (a andb) —H —Br Q15 (a and b) —H —I Q16 (a and b) —H -n-butyl Q17 (a and b) —H—CH₃ Q18 (a and b) —H —SCF₃ Q19 (a and b) —H —N(CH₂CH₃)₂ Q20 (a and b)—H —OCF₂CHF₂ Q21 (a and b) —H —C(OH)(CF₃)₂ Q22 (a and b) —H-(1,1-dimethyl-pentyl) Q23 (a and b) —H -(1,1-dimethyl-acetic acid)ethyl ester Q24 (a and b) —H —N-piperidinyl Q25 (a and b) —Cl —H Q26 (aand b) —Cl -tert-butyl Q27 (a and b) —Cl -iso-butyl Q28 (a and b) —Cl-sec-butyl Q29 (a and b) —Cl -iso-propyl Q30 (a and b) —Cl -n-propyl Q31(a and b) —Cl -cyclohexyl Q32 (a and b) —Cl -tert-butoxy Q33 (a and b)—Cl -isopropoxy Q34 (a and b) —Cl —CF₃ Q35 (a and b) —Cl —CH₂CF₃ Q36 (aand b) —Cl —OCF₃ Q37 (a and b) —Cl —Cl Q38 (a and b) —Cl —Br Q39 (a andb) —Cl —I Q40 (a and b) —Cl -n-butyl Q41 (a and b) —Cl —CH₃ Q42 (a andb) —Cl —SCF₃ Q43 (a and b) —Cl —N(CH₂CH₃)₂ Q44 (a and b) —Cl —OCF₂CHF₂Q45 (a and b) —Cl —C(OH)(CF₃)₂ Q46 (a and b) —Cl -(1,1-dimethyl-pentyl)Q47 (a and b) —Cl -(1,1-dimethyl-acetic acid) ethyl ester Q48 (a and b)—Cl —N-piperidinyl Q49 (a and b) —F —H Q50 (a and b) —F -tert-butyl Q51(a and b) —F -iso-butyl Q52 (a and b) —F -sec-butyl Q53 (a and b) —F-iso-propyl Q54 (a and b) —F -n-propyl Q55 (a and b) —F -cyclohexyl Q56(a and b) —F -tert-butoxy Q57 (a and b) —F -isopropoxy Q58 (a and b) —F—CF₃ Q59 (a and b) —F —CH₂CF₃ Q60 (a and b) —F —OCF₃ Q61 (a and b) —F—Cl Q62 (a and b) —F —Br Q63 (a and b) —F —I Q64 (a and b) —F -n-butylQ65 (a and b) —F —CH₃ Q66 (a and b) —F —SCF₃ Q67 (a and b) —F—N(CH₂CH₃)₂ Q68 (a and b) —F —OCF₂CHF₂ Q69 (a and b) —F —C(OH)(CF₃)₂ Q70(a and b) —F -(1,1-dimethyl-pentyl) Q71 (a and b) —F-(1,1-dimethyl-acetic acid) ethyl ester Q72 (a and b) —F —N-piperidinylQ73 (a and b) —CH₃ —H Q74 (a and b) —CH₃ -iso-butyl Q75 (a and b) —CH₃-tert-butyl Q76 (a and b) —CH₃ -sec-butyl Q77 (a and b) —CH₃ -iso-propylQ78 (a and b) —CH₃ -n-propyl Q79 (a and b) —CH₃ -cyclohexyl Q80 (a andb) —CH₃ -tert-butoxy Q81 (a and b) —CH₃ -isopropoxy Q82 (a and b) —CH₃—CF₃ Q83 (a and b) —CH₃ —CH₂CF₃ Q84 (a and b) —CH₃ —OCF₃ Q85 (a and b)—CH₃ —Cl Q86 (a and b) —CH₃ —Br Q87 (a and b) —CH₃ —I Q88 (a and b) —CH₃-n-butyl Q89 (a and b) —CH₃ —CH₃ Q90 (a and b) —CH₃ —SCF₃ Q91 (a and b)—CH₃ —N(CH₂CH₃)₂ Q92 (a and b) —CH₃ —OCF₂CHF₂ Q93 (a and b) —CH₃—C(OH)(CF₃)₂ Q94 (a and b) —CH₃ -(1,1-dimethyl-pentyl) Q95 (a and b)—CH₃ -(1,1-dimethyl-acetic acid) ethyl ester Q96 (a and b) —CH₃—N-piperidinyl Q97 (a and b) —CF₃ —H Q98 (a and b) —CF₃ -tert-butyl Q99(a and b) —CF₃ -iso-butyl Q100 (a and b) —CF₃ -sec-butyl Q101 (a and b)—CF₃ -iso-propyl Q102 (a and b) —CF₃ -n-propyl Q103 (a and b) —CF₃-cyclohexyl Q104 (a and b) —CF₃ -tert-butoxy Q105 (a and b) —CF₃-isopropoxy Q106 (a and b) —CF₃ —CF₃ Q107 (a and b) —CF₃ —CH₂CF₃ Q108 (aand b) —CF₃ —OCF₃ Q109 (a and b) —CF₃ —Cl Q110 (a and b) —CF₃ —Br Q111(a and b) —CF₃ —I Q112 (a and b) —CF₃ -n-butyl Q113 (a and b) —CF₃ —CH₃Q114 (a and b) —CF₃ —SCF₃ Q115 (a and b) —CF₃ —N(CH₂CH₃)₂ Q116 (a and b)—CF₃ —OCF₂CHF₂ Q117 (a and b) —CF₃ —C(OH)(CF₃)₂ Q118 (a and b) —CF₃-(1,1-dimethyl-pentyl) Q119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester Q120 (a and b) —CF₃ —N-piperidinyl Q121 (a and b) —CHF₂-tert-butyl Q122 (a and b) —CHF₂ —H Q123 (a and b) —CHF₂ -iso-butyl Q124(a and b) —CHF₂ -sec-butyl Q125 (a and b) —CHF₂ -iso-propyl Q126 (a andb) —CHF₂ -n-propyl Q127 (a and b) —CHF₂ -cyclohexyl Q128 (a and b) —CHF₂-tert-butoxy Q129 (a and b) —CHF₂ -isopropoxy Q130 (a and b) —CHF₂ —CF₃Q131 (a and b) —CHF₂ —CH₂CF₃ Q132 (a and b) —CHF₂ —OCF₃ Q133 (a and b)—CHF₂ —Cl Q134 (a and b) —CHF₂ —Br Q135 (a and b) —CHF₂ —I Q136 (a andb) —CHF₂ -n-butyl Q137 (a and b) —CHF₂ —CH₃ Q138 (a and b) —CHF₂ —SCF₃Q139 (a and b) —CHF₂ —N(CH₂CH₃)₂ Q140 (a and b) —CHF₂ —OCF₂CHF₂ Q141 (aand b) —CHF₂ —C(OH)(CF₃)₂ Q142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)Q143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester Q144 (a andb) —CHF₂ —N-piperidinyl Q145 (a and b) —OH —H Q146 (a and b) —OH-tert-butyl Q147 (a and b) —OH -iso-butyl Q148 (a and b) —OH -sec-butylQ149 (a and b) —OH -iso-propyl Q150 (a and b) —OH -n-propyl Q151 (a andb) —OH -cyclohexyl Q152 (a and b) —OH -tert-butoxy Q153 (a and b) —OH-isopropoxy Q154 (a and b) —OH —CF₃ Q155 (a and b) —OH —CH₂CF₃ Q156 (aand b) —OH —OCF₃ Q157 (a and b) —OH —Cl Q158 (a and b) —OH —Br Q159 (aand b) —OH —I Q160 (a and b) —OH -n-butyl Q161 (a and b) —OH —CH₃ Q162(a and b) —OH —SCF₃ Q163 (a and b) —OH —N(CH₂CH₃)₂ Q164 (a and b) —OH—OCF₂CHF₂ Q165 (a and b) —OH —C(OH)(CF₃)₂ Q166 (a and b) —OH-(1,1-dimethyl-pentyl) Q167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester Q168 (a and b) —OH —N-piperidinyl Q169 (a and b) —NO₂ —HQ170 (a and b) —NO₂ -tert-butyl Q171 (a and b) —NO₂ -iso-butyl Q172 (aand b) —NO₂ -sec-butyl Q173 (a and b) —NO₂ -iso-propyl Q174 (a and b)—NO₂ -n-propyl Q175 (a and b) —NO₂ -cyclohexyl Q176 (a and b) —NO₂-tert-butoxy Q177 (a and b) —NO₂ -isopropoxy Q178 (a and b) —NO₂ —CF₃Q179 (a and b) —NO₂ —CH₂CF₃ Q180 (a and b) —NO₂ —OCF₃ Q181 (a and b)—NO₂ —Cl Q182 (a and b) —NO₂ —Br Q183 (a and b) —NO₂ —I Q184 (a and b)—NO₂ -n-butyl Q185 (a and b) —NO₂ —CH₃ Q186 (a and b) —NO₂ —SCF₃ Q187 (aand b) —NO₂ —N(CH₂CH₃)₂ Q188 (a and b) —NO₂ —OCF₂CHF₂ Q189 (a and b)—NO₂ —C(OH)(CF₃)₂ Q190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) Q191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester Q192 (a and b) —NO₂—N-piperidinyl Q193 (a and b) —CN —H Q194 (a and b) —CN -tert-butyl Q195(a and b) —CN -iso-butyl Q196 (a and b) —CN -sec-butyl Q197 (a and b)—CN -iso-propyl Q198 (a and b) —CN -n-propyl Q199 (a and b) —CN-cyclohexyl Q200 (a and b) —CN -tert-butoxy Q201 (a and b) —CN-isopropoxy Q202 (a and b) —CN —CF₃ Q203 (a and b) —CN —CH₂CF₃ Q204 (aand b) —CN —OCF₃ Q205 (a and b) —CN —Cl Q206 (a and b) —CN —Br Q207 (aand b) —CN —I Q208 (a and b) —CN -n-butyl Q209 (a and b) —CN —CH₃ Q210(a and b) —CN —SCF₃ Q211 (a and b) —CN —N(CH₂CH₃)₂ Q212 (a and b) —CN—OCF₂CHF₂ Q213 (a and b) —CN —C(OH)(CF₃)₂ Q214 (a and b) —CN-(1,1-dimethyl-pentyl) Q215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester Q216 (a and b) —CN —N-piperidinyl Q217 (a and b) —Br —H Q218(a and b) —Br -tert-butyl Q219 (a and b) —Br -iso-butyl Q220 (a and b)—Br -sec-butyl Q221 (a and b) —Br -iso-propyl Q222 (a and b) —Br-n-propyl Q223 (a and b) —Br -cyclohexyl Q224 (a and b) —Br -tert-butoxyQ225 (a and b) —Br -isopropoxy Q226 (a and b) —Br —CF₃ Q227 (a and b)—Br —CH₂CF₃ Q228 (a and b) —Br —OCF₃ Q229 (a and b) —Br —Cl Q230 (a andb) —Br —Br Q231 (a and b) —Br —I Q232 (a and b) —Br -n-butyl Q233 (a andb) —Br —CH₃ Q234 (a and b) —Br —SCF₃ Q235 (a and b) —Br —N(CH₂CH₃)₂ Q236(a and b) —Br —OCF₂CHF₂ Q237 (a and b) —Br —C(OH)(CF₃)₂ Q238 (a and b)—Br -(1,1-dimethyl-pentyl) Q239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester Q240 (a and b) —Br —N-piperidinyl Q241 (a and b) —I-tert-butyl Q242 (a and b) —I —H Q243 (a and b) —I -iso-butyl Q244 (aand b) —I -sec-butyl Q245 (a and b) —I -iso-propyl Q246 (a and b) —I-n-propyl Q247 (a and b) —I -cyclohexyl Q248 (a and b) —I -tert-butoxyQ249 (a and b) —I -isopropoxy Q250 (a and b) —I —CF₃ Q251 (a and b) —I—CH₂CF₃ Q252 (a and b) —I —OCF₃ Q253 (a and b) —I —Cl Q254 (a and b) —I—Br Q255 (a and b) —I —I Q256 (a and b) —I -n-butyl Q257 (a and b) —I—CH₃ Q258 (a and b) —I —SCF₃ Q259 (a and b) —I —N(CH₂CH₃)₂ Q260 (a andb) —I —OCF₂CHF₂ Q261 (a and b) —I —C(OH)(CF₃)₂ Q262 (a and b) —I-(1,1-dimethyl-pentyl) Q263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester Q264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 18 (Ir)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  R1 (a and b) —H —H  R2 (a and b) —H -tert-butyl  R3 (a and b) —H-iso-butyl  R4 (a and b) —H -sec-butyl  R5 (a and b) —H -iso-propyl  R6(a and b) —H -n-propyl  R7 (a and b) —H -cyclohexyl  R8 (a and b) —H-tert-butoxy  R9 (a and b) —H -isopropoxy  R10 (a and b) —H —CF₃  R11 (aand b) —H —CH₂CF₃  R12 (a and b) —H —OCF₃  R13 (a and b) —H —Cl  R14 (aand b) —H —Br  R15 (a and b) —H —I  R16 (a and b) —H -n-butyl  R17 (aand b) —H —CH₃  R18 (a and b) —H —SCF₃  R19 (a and b) —H —N(CH₂CH₃)₂ R20 (a and b) —H —OCF₂CHF₂  R21 (a and b) —H —C(OH)(CF₃)₂  R22 (a andb) —H -(1,1-dimethyl-pentyl)  R23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester  R24 (a and b) —H —N-piperidinyl  R25 (a and b) —Cl —H R26 (a and b) —Cl -tert-butyl  R27 (a and b) —Cl -iso-butyl  R28 (a andb) —Cl -sec-butyl  R29 (a and b) —Cl -iso-propyl  R30 (a and b) —Cl-n-propyl  R31 (a and b) —Cl -cyclohexyl  R32 (a and b) —Cl -tert-butoxy R33 (a and b) —Cl -isopropoxy  R34 (a and b) —Cl —CF₃  R35 (a and b)—Cl —CH₂CF₃  R36 (a and b) —Cl —OCF₃  R37 (a and b) —Cl —Cl  R38 (a andb) —Cl —Br  R39 (a and b) —Cl —I  R40 (a and b) —Cl -n-butyl  R41 (a andb) —Cl —CH₃  R42 (a and b) —Cl —SCF₃  R43 (a and b) —Cl —N(CH₂CH₃)₂  R44(a and b) —Cl —OCF₂CHF₂  R45 (a and b) —Cl —C(OH)(CF₃)₂  R46 (a and b)—Cl -(1,1-dimethyl-pentyl)  R47 (a and b) —Cl -(1,1-dimethyl-aceticacid) ethyl ester  R48 (a and b) —Cl —N-piperidinyl  R49 (a and b) —F —H R50 (a and b) —F -tert-butyl  R51 (a and b) —F -iso-butyl  R52 (a andb) —F -sec-butyl  R53 (a and b) —F -iso-propyl  R54 (a and b) —F-n-propyl  R55 (a and b) —F -cyclohexyl  R56 (a and b) —F -tert-butoxy R57 (a and b) —F -isopropoxy  R58 (a and b) —F —CF₃  R59 (a and b) —F—CH₂CF₃  R60 (a and b) —F —OCF₃  R61 (a and b) —F —Cl  R62 (a and b) —F—Br  R63 (a and b) —F —I  R64 (a and b) —F -n-butyl  R65 (a and b) —F—CH₃  R66 (a and b) —F —SCF₃  R67 (a and b) —F —N(CH₂CH₃)₂  R68 (a andb) —F —OCF₂CHF₂  R69 (a and b) —F —C(OH)(CF₃)₂  R70 (a and b) —F-(1,1-dimethyl-pentyl)  R71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester  R72 (a and b) —F —N-piperidinyl  R73 (a and b) —CH₃ —H  R74(a and b) —CH₃ -iso-butyl  R75 (a and b) —CH₃ -tert-butyl  R76 (a and b)—CH₃ -sec-butyl  R77 (a and b) —CH₃ -iso-propyl  R78 (a and b) —CH₃-n-propyl  R79 (a and b) —CH₃ -cyclohexyl  R80 (a and b) —CH₃-tert-butoxy  R81 (a and b) —CH₃ -isopropoxy  R82 (a and b) —CH₃ —CF₃ R83 (a and b) —CH₃ —CH₂CF₃  R84 (a and b) —CH₃ —OCF₃  R85 (a and b)—CH₃ —Cl  R86 (a and b) —CH₃ —Br  R87 (a and b) —CH₃ —I  R88 (a and b)—CH₃ -n-butyl  R89 (a and b) —CH₃ —CH₃  R90 (a and b) —CH₃ —SCF₃  R91 (aand b) —CH₃ —N(CH₂CH₃)₂  R92 (a and b) —CH₃ —OCF₂CHF₂  R93 (a and b)—CH₃ —C(OH)(CF₃)₂  R94 (a and b) —CH₃ -(1,1-dimethyl-pentyl)  R95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester  R96 (a and b) —CH₃—N-piperidinyl  R97 (a and b) —CF₃ —H  R98 (a and b) —CF₃ -tert-butyl R99 (a and b) —CF₃ -iso-butyl R100 (a and b) —CF₃ -sec-butyl R101 (aand b) —CF₃ -iso-propyl R102 (a and b) —CF₃ -n-propyl R103 (a and b)—CF₃ -cyclohexyl R104 (a and b) —CF₃ -tert-butoxy R105 (a and b) —CF₃-isopropoxy R106 (a and b) —CF₃ —CF₃ R107 (a and b) —CF₃ —CH₂CF₃ R108 (aand b) —CF₃ —OCF₃ R109 (a and b) —CF₃ —Cl R110 (a and b) —CF₃ —Br R111(a and b) —CF₃ —I R112 (a and b) —CF₃ -n-butyl R113 (a and b) —CF₃ —CH₃R114 (a and b) —CF₃ —SCF₃ R115 (a and b) —CF₃ —N(CH₂CH₃)₂ R116 (a and b)—CF₃ —OCF₂CHF₂ R117 (a and b) —CF₃ —C(OH)(CF₃)₂ R118 (a and b) —CF₃-(1,1-dimethyl-pentyl) R119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester R120 (a and b) —CF₃ —N-piperidinyl R121 (a and b) —CHF₂-tert-butyl R122 (a and b) —CHF₂ —H R123 (a and b) —CHF₂ -iso-butyl R124(a and b) —CHF₂ -sec-butyl R125 (a and b) —CHF₂ -iso-propyl R126 (a andb) —CHF₂ -n-propyl R127 (a and b) —CHF₂ -cyclohexyl R128 (a and b) —CHF₂-tert-butoxy R129 (a and b) —CHF₂ -isopropoxy R130 (a and b) —CHF₂ —CF₃R131 (a and b) —CHF₂ —CH₂CF₃ R132 (a and b) —CHF₂ —OCF₃ R133 (a and b)—CHF₂ —Cl R134 (a and b) —CHF₂ —Br R135 (a and b) —CHF₂ —I R136 (a andb) —CHF₂ -n-butyl R137 (a and b) —CHF₂ —CH₃ R138 (a and b) —CHF₂ —SCF₃R139 (a and b) —CHF₂ —N(CH₂CH₃)₂ R140 (a and b) —CHF₂ —OCF₂CHF₂ R141 (aand b) —CHF₂ —C(OH)(CF₃)₂ R142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)R143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester R144 (a andb) —CHF₂ —N-piperidinyl R145 (a and b) —OH —H R146 (a and b) —OH-tert-butyl R147 (a and b) —OH -iso-butyl R148 (a and b) —OH -sec-butylR149 (a and b) —OH -iso-propyl R150 (a and b) —OH -n-propyl R151 (a andb) —OH -cyclohexyl R152 (a and b) —OH -tert-butoxy R153 (a and b) —OH-isopropoxy R154 (a and b) —OH —CF₃ R155 (a and b) —OH —CH₂CF₃ R156 (aand b) —OH —OCF₃ R157 (a and b) —OH —Cl R158 (a and b) —OH —Br R159 (aand b) —OH —I R160 (a and b) —OH -n-butyl R161 (a and b) —OH —CH₃ R162(a and b) —OH —SCF₃ R163 (a and b) —OH —N(CH₂CH₃)₂ R164 (a and b) —OH—OCF₂CHF₂ R165 (a and b) —OH —C(OH)(CF₃)₂ R166 (a and b) —OH-(1,1-dimethyl-pentyl) R167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester R168 (a and b) —OH —N-piperidinyl R169 (a and b) —NO₂ —HR170 (a and b) —NO₂ -tert-butyl R171 (a and b) —NO₂ -iso-butyl R172 (aand b) —NO₂ -sec-butyl R173 (a and b) —NO₂ -iso-propyl R174 (a and b)—NO₂ -n-propyl R175 (a and b) —NO₂ -cyclohexyl R176 (a and b) —NO₂-tert-butoxy R177 (a and b) —NO₂ -isopropoxy R178 (a and b) —NO₂ —CF₃R179 (a and b) —NO₂ —CH₂CF₃ R180 (a and b) —NO₂ —OCF₃ R181 (a and b)—NO₂ —Cl R182 (a and b) —NO₂ —Br R183 (a and b) —NO₂ —I R184 (a and b)—NO₂ -n-butyl R185 (a and b) —NO₂ —CH₃ R186 (a and b) —NO₂ —SCF₃ R187 (aand b) —NO₂ —N(CH₂CH₃)₂ R188 (a and b) —NO₂ —OCF₂CHF₂ R189 (a and b)—NO₂ —C(OH)(CF₃)₂ R190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) R191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester R192 (a and b) —NO₂—N-piperidinyl R193 (a and b) —CN —H R194 (a and b) —CN -tert-butyl R195(a and b) —CN -iso-butyl R196 (a and b) —CN -sec-butyl R197 (a and b)—CN -iso-propyl R198 (a and b) —CN -n-propyl R199 (a and b) —CN-cyclohexyl R200 (a and b) —CN -tert-butoxy R201 (a and b) —CN-isopropoxy R202 (a and b) —CN —CF₃ R203 (a and b) —CN —CH₂CF₃ R204 (aand b) —CN —OCF₃ R205 (a and b) —CN —Cl R206 (a and b) —CN —Br R207 (aand b) —CN —I R208 (a and b) —CN -n-butyl R209 (a and b) —CN —CH₃ R210(a and b) —CN —SCF₃ R211 (a and b) —CN —N(CH₂CH₃)₂ R212 (a and b) —CN—OCF₂CHF₂ R213 (a and b) —CN —C(OH)(CF₃)₂ R214 (a and b) —CN-(1,1-dimethyl-pentyl) R215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester R216 (a and b) —CN —N-piperidinyl R217 (a and b) —Br —H R218(a and b) —Br -tert-butyl R219 (a and b) —Br -iso-butyl R220 (a and b)—Br -sec-butyl R221 (a and b) —Br -iso-propyl R222 (a and b) —Br-n-propyl R223 (a and b) —Br -cyclohexyl R224 (a and b) —Br -tert-butoxyR225 (a and b) —Br -isopropoxy R226 (a and b) —Br —CF₃ R227 (a and b)—Br —CH₂CF₃ R228 (a and b) —Br —OCF₃ R229 (a and b) —Br —Cl R230 (a andb) —Br —Br R231 (a and b) —Br —I R232 (a and b) —Br -n-butyl R233 (a andb) —Br —CH₃ R234 (a and b) —Br —SCF₃ R235 (a and b) —Br —N(CH₂CH₃)₂ R236(a and b) —Br —OCF₂CHF₂ R237 (a and b) —Br —C(OH)(CF₃)₂ R238 (a and b)—Br -(1,1-dimethyl-pentyl) R239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester R240 (a and b) —Br —N-piperidinyl R241 (a and b) —I-tert-butyl R242 (a and b) —I —H R243 (a and b) —I -iso-butyl R244 (aand b) —I -sec-butyl R245 (a and b) —I -iso-propyl R246 (a and b) —I-n-propyl R247 (a and b) —I -cyclohexyl R248 (a and b) —I -tert-butoxyR249 (a and b) —I -isopropoxy R250 (a and b) —I —CF₃ R251 (a and b) —I—CH₂CF₃ R252 (a and b) —I —OCF₃ R253 (a and b) —I —Cl R254 (a and b) —I—Br R255 (a and b) —I —I R256 (a and b) —I -n-butyl R257 (a and b) —I—CH₃ R258 (a and b) —I —SCF₃ R259 (a and b) —I —N(CH₂CH₃)₂ R260 (a andb) —I —OCF₂CHF₂ R261 (a and b) —I —C(OH)(CF₃)₂ R262 (a and b) —I-(1,1-dimethyl-pentyl) R263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester R264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 19 (Is)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  S1 (a and b) —H —H  S2 (a and b) —H -tert-butyl  S3 (a and b) —H-iso-butyl  S4 (a and b) —H -sec-butyl  S5 (a and b) —H -iso-propyl  S6(a and b) —H -n-propyl  S7 (a and b) —H -cyclohexyl  S8 (a and b) —H-tert-butoxy  S9 (a and b) —H -isopropoxy  S10 (a and b) —H —CF₃  S11 (aand b) —H —CH₂CF₃  S12 (a and b) —H —OCF₃  S13 (a and b) —H —Cl  S14 (aand b) —H —Br  S15 (a and b) —H —I  S16 (a and b) —H -n-butyl  S17 (aand b) —H —CH₃  S18 (a and b) —H —SCF₃  S19 (a and b) —H —N(CH₂CH₃)₂ S20 (a and b) —H —OCF₂CHF₂  S21 (a and b) —H —C(OH)(CF₃)₂  S22 (a andb) —H -(1,1-dimethyl-pentyl)  S23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester  S24 (a and b) —H —N-piperidinyl  S25 (a and b) —Cl —H S26 (a and b) —Cl -tert-butyl  S27 (a and b) —Cl -iso-butyl  S28 (a andb) —Cl -sec-butyl  S29 (a and b) —Cl -iso-propyl  S30 (a and b) —Cl-n-propyl  S31 (a and b) —Cl -cyclohexyl  S32 (a and b) —Cl -tert-butoxy S33 (a and b) —Cl -isopropoxy  S34 (a and b) —Cl —CF₃  S35 (a and b)—Cl —CH₂CF₃  S36 (a and b) —Cl —OCF₃  S37 (a and b) —Cl —Cl  S38 (a andb) —Cl —Br  S39 (a and b) —Cl —I  S40 (a and b) —Cl -n-butyl  S41 (a andb) —Cl —CH₃  S42 (a and b) —Cl —SCF₃  S43 (a and b) —Cl —N(CH₂CH₃)₂  S44(a and b) —Cl —OCF₂CHF₂  S45 (a and b) —Cl —C(OH)(CF₃)₂  S46 (a and b)—Cl -(1,1-dimethyl-pentyl)  S47 (a and b) —Cl -(1,1-dimethyl-aceticacid) ethyl ester  S48 (a and b) —Cl —N-piperidinyl  S49 (a and b) —F —H S50 (a and b) —F -tert-butyl  S51 (a and b) —F -iso-butyl  S52 (a andb) —F -sec-butyl  S53 (a and b) —F -iso-propyl  S54 (a and b) —F-n-propyl  S55 (a and b) —F -cyclohexyl  S56 (a and b) —F -tert-butoxy S57 (a and b) —F -isopropoxy  S58 (a and b) —F —CF₃  S59 (a and b) —F—CH₂CF₃  S60 (a and b) —F —OCF₃  S61 (a and b) —F —Cl  S62 (a and b) —F—Br  S63 (a and b) —F —I  S64 (a and b) —F -n-butyl  S65 (a and b) —F—CH₃  S66 (a and b) —F —SCF₃  S67 (a and b) —F —N(CH₂CH₃)₂  S68 (a andb) —F —OCF₂CHF₂  S69 (a and b) —F —C(OH)(CF₃)₂  S70 (a and b) —F-(1,1-dimethyl-pentyl)  S71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester  S72 (a and b) —F —N-piperidinyl  S73 (a and b) —CH₃ —H  S74(a and b) —CH₃ -iso-butyl  S75 (a and b) —CH₃ -tert-butyl  S76 (a and b)—CH₃ -sec-butyl  S77 (a and b) —CH₃ -iso-propyl  S78 (a and b) —CH₃-n-propyl  S79 (a and b) —CH₃ -cyclohexyl  S80 (a and b) —CH₃-tert-butoxy  S81 (a and b) —CH₃ -isopropoxy  S82 (a and b) —CH₃ —CF₃ S83 (a and b) —CH₃ —CH₂CF₃  S84 (a and b) —CH₃ —OCF₃  S85 (a and b)—CH₃ —Cl  S86 (a and b) —CH₃ —Br  S87 (a and b) —CH₃ —I  S88 (a and b)—CH₃ -n-butyl  S89 (a and b) —CH₃ —CH₃  S90 (a and b) —CH₃ —SCF₃  S91 (aand b) —CH₃ —N(CH₂CH₃)₂  S92 (a and b) —CH₃ —OCF₂CHF₂  S93 (a and b)—CH₃ —C(OH)(CF₃)₂  S94 (a and b) —CH₃ -(1,1-dimethyl-pentyl)  S95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester  S96 (a and b) —CH₃—N-piperidinyl  S97 (a and b) —CF₃ —H  S98 (a and b) —CF₃ -tert-butyl S99 (a and b) —CF₃ -iso-butyl S100 (a and b) —CF₃ -sec-butyl S101 (aand b) —CF₃ -iso-propyl S102 (a and b) —CF₃ -n-propyl S103 (a and b)—CF₃ -cyclohexyl S104 (a and b) —CF₃ -tert-butoxy S105 (a and b) —CF₃-isopropoxy S106 (a and b) —CF₃ —CF₃ S107 (a and b) —CF₃ —CH₂CF₃ S108 (aand b) —CF₃ —OCF₃ S109 (a and b) —CF₃ —Cl S110 (a and b) —CF₃ —Br S111(a and b) —CF₃ —I S112 (a and b) —CF₃ -n-butyl S113 (a and b) —CF₃ —CH₃S114 (a and b) —CF₃ —SCF₃ S115 (a and b) —CF₃ —N(CH₂CH₃)₂ S116 (a and b)—CF₃ —OCF₂CHF₂ S117 (a and b) —CF₃ —C(OH)(CF₃)₂ S118 (a and b) —CF₃-(1,1-dimethyl-pentyl) S119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester S120 (a and b) —CF₃ —N-piperidinyl S121 (a and b) —CHF₂-tert-butyl S122 (a and b) —CHF₂ —H S123 (a and b) —CHF₂ -iso-butyl S124(a and b) —CHF₂ -sec-butyl S125 (a and b) —CHF₂ -iso-propyl S126 (a andb) —CHF₂ -n-propyl S127 (a and b) —CHF₂ -cyclohexyl S128 (a and b) —CHF₂-tert-butoxy S129 (a and b) —CHF₂ -isopropoxy S130 (a and b) —CHF₂ —CF₃S131 (a and b) —CHF₂ —CH₂CF₃ S132 (a and b) —CHF₂ —OCF₃ S133 (a and b)—CHF₂ —Cl S134 (a and b) —CHF₂ —Br S135 (a and b) —CHF₂ —I S136 (a andb) —CHF₂ -n-butyl S137 (a and b) —CHF₂ —CH₃ S138 (a and b) —CHF₂ —SCF₃S139 (a and b) —CHF₂ —N(CH₂CH₃)₂ S140 (a and b) —CHF₂ —OCF₂CHF₂ S141 (aand b) —CHF₂ —C(OH)(CF₃)₂ S142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)S143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester S144 (a andb) —CHF₂ —N-piperidinyl S145 (a and b) —OH —H S146 (a and b) —OH-tert-butyl S147 (a and b) —OH -iso-butyl S148 (a and b) —OH -sec-butylS149 (a and b) —OH -iso-propyl S150 (a and b) —OH -n-propyl S151 (a andb) —OH -cyclohexyl S152 (a and b) —OH -tert-butoxy S153 (a and b) —OH-isopropoxy S154 (a and b) —OH —CF₃ S155 (a and b) —OH —CH₂CF₃ S156 (aand b) —OH —OCF₃ S157 (a and b) —OH —Cl S158 (a and b) —OH —Br S159 (aand b) —OH —I S160 (a and b) —OH -n-butyl S161 (a and b) —OH —CH₃ S162(a and b) —OH —SCF₃ S163 (a and b) —OH —N(CH₂CH₃)₂ S164 (a and b) —OH—OCF₂CHF₂ S165 (a and b) —OH —C(OH)(CF₃)₂ S166 (a and b) —OH-(1,1-dimethyl-pentyl) S167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester S168 (a and b) —OH —N-piperidinyl S169 (a and b) —NO₂ —HS170 (a and b) —NO₂ -tert-butyl S171 (a and b) —NO₂ -iso-butyl S172 (aand b) —NO₂ -sec-butyl S173 (a and b) —NO₂ -iso-propyl S174 (a and b)—NO₂ -n-propyl S175 (a and b) —NO₂ -cyclohexyl S176 (a and b) —NO₂-tert-butoxy S177 (a and b) —NO₂ -isopropoxy S178 (a and b) —NO₂ —CF₃S179 (a and b) —NO₂ —CH₂CF₃ S180 (a and b) —NO₂ —OCF₃ S181 (a and b)—NO₂ —Cl S182 (a and b) —NO₂ —Br S183 (a and b) —NO₂ —I S184 (a and b)—NO₂ -n-butyl S185 (a and b) —NO₂ —CH₃ S186 (a and b) —NO₂ —SCF₃ S187 (aand b) —NO₂ —N(CH₂CH₃)₂ S188 (a and b) —NO₂ —OCF₂CHF₂ S189 (a and b)—NO₂ —C(OH)(CF₃)₂ S190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) S191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester S192 (a and b) —NO₂—N-piperidinyl S193 (a and b) —CN —H S194 (a and b) —CN -tert-butyl S195(a and b) —CN -iso-butyl S196 (a and b) —CN -sec-butyl S197 (a and b)—CN -iso-propyl S198 (a and b) —CN -n-propyl S199 (a and b) —CN-cyclohexyl S200 (a and b) —CN -tert-butoxy S201 (a and b) —CN-isopropoxy S202 (a and b) —CN —CF₃ S203 (a and b) —CN —CH₂CF₃ S204 (aand b) —CN —OCF₃ S205 (a and b) —CN —Cl S206 (a and b) —CN —Br S207 (aand b) —CN —I S208 (a and b) —CN -n-butyl S209 (a and b) —CN —CH₃ S210(a and b) —CN —SCF₃ S211 (a and b) —CN —N(CH₂CH₃)₂ S212 (a and b) —CN—OCF₂CHF₂ S213 (a and b) —CN —C(OH)(CF₃)₂ S214 (a and b) —CN-(1,1-dimethyl-pentyl) S215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester S216 (a and b) —CN —N-piperidinyl S217 (a and b) —Br —H S218(a and b) —Br -tert-butyl S219 (a and b) —Br -iso-butyl S220 (a and b)—Br -sec-butyl S221 (a and b) —Br -iso-propyl S222 (a and b) —Br-n-propyl S223 (a and b) —Br -cyclohexyl S224 (a and b) —Br -tert-butoxyS225 (a and b) —Br -isopropoxy S226 (a and b) —Br —CF₃ S227 (a and b)—Br —CH₂CF₃ S228 (a and b) —Br —OCF₃ S229 (a and b) —Br —Cl S230 (a andb) —Br —Br S231 (a and b) —Br —I S232 (a and b) —Br -n-butyl S233 (a andb) —Br —CH₃ S234 (a and b) —Br —SCF₃ S235 (a and b) —Br —N(CH₂CH₃)₂ S236(a and b) —Br —OCF₂CHF₂ S237 (a and b) —Br —C(OH)(CF₃)₂ S238 (a and b)—Br -(1,1-dimethyl-pentyl) S239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester S240 (a and b) —Br —N-piperidinyl S241 (a and b) —I-tert-butyl S242 (a and b) —I —H S243 (a and b) —I -iso-butyl S244 (aand b) —I -sec-butyl S245 (a and b) —I -iso-propyl S246 (a and b) —I-n-propyl S247 (a and b) —I -cyclohexyl S248 (a and b) —I -tert-butoxyS249 (a and b) —I -isopropoxy S250 (a and b) —I —CF₃ S251 (a and b) —I—CH₂CF₃ S252 (a and b) —I —OCF₃ S253 (a and b) —I —Cl S254 (a and b) —I—Br S255 (a and b) —I —I S256 (a and b) —I -n-butyl S257 (a and b) —I—CH₃ S258 (a and b) —I —SCF₃ S259 (a and b) —I —N(CH₂CH₃)₂ S260 (a andb) —I —OCF₂CHF₂ S261 (a and b) —I —C(OH)(CF₃)₂ S262 (a and b) —I-(1,1-dimethyl-pentyl) S263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester S264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 20 (It)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b)  T1 (a and b) S —H —Cl —H  T2 (a and b) S —H —Br —H T3 (a and b) S —H —F —H  T4 (a and b) S —H —CH₃ —H  T5 (a and b) S —H—CF₃ —H  T6 (a and b) S —H —OCH₃ —H  T7 (a and b) S —H —OCH₂CH₃ —H  T8(a and b) S —H —OCF₃ —H  T9 (a and b) S —H -tert-butyl —H  T10 (a and b)S —H -iso-propyl —H  T11 (a and b) S —H —CH₃ —CH₃  T12 (a and b) S —H —H—H  T13 (a and b) S —H —H —Cl  T14 (a and b) S —H —H —Br  T15 (a and b)S —H —H —F  T16 (a and b) S —H —H —CH₃  T17 (a and b) S —H —H —CF₃  T18(a and b) S —H —H —OCH₃  T19 (a and b) S —H —H —OCH₂CH₃  T20 (a and b) S—H —H —OCF₃  T21 (a and b) S —H —H -tert-butyl  T22 (a and b) S —H —H-iso-propyl  T23 (a and b) S —Cl —Cl —H  T24 (a and b) S —Cl —Br —H  T25(a and b) S —Cl —F —H  T26 (a and b) S —Cl —CH₃ —H  T27 (a and b) S —Cl—CF₃ —H  T28 (a and b) S —Cl —OCH₃ —H  T29 (a and b) S —Cl —OCH₂CH₃ —H T30 (a and b) S —Cl —OCF₃ —H  T31 (a and b) S —Cl -tert-butyl —H  T32(a and b) S —Cl -iso-propyl —H  T33 (a and b) S —Cl —CH₃ —CH₃  T34 (aand b) S —Cl —H —H  T35 (a and b) S —Cl —H —Cl  T36 (a and b) S —Cl —H—Br  T37 (a and b) S —Cl —H —F  T38 (a and b) S —Cl —H —CH₃  T39 (a andb) S —Cl —H —CF₃  T40 (a and b) S —Cl —H —OCH₃  T41 (a and b) S —Cl —H—OCH₂CH₃  T42 (a and b) S —Cl —H —OCF₃  T43 (a and b) S —Cl —H-tert-butyl  T44 (a and b) S —Cl —H -iso-propyl  T45 (a and b) S —Cl —H—OCF₃  T46 (a and b) S —Cl —H -tert-butyl  T47 (a and b) S —Cl —H-iso-propyl  T48 (a and b) S —CH₃ —Cl —H  T49 (a and b) S —CH₃ —Br —H T50 (a and b) S —CH₃ —F —H  T51 (a and b) S —CH₃ —CH₃ —H  T52 (a and b)S —CH₃ —CF₃ —H  T53 (a and b) S —CH₃ —OCH₃ —H  T54 (a and b) S —CH₃—OCH₂CH₃ —H  T55 (a and b) S —CH₃ —OCF₃ —H  T56 (a and b) S —CH₃-tert-butyl —H  T57 (a and b) S —CH₃ -iso-propyl —H  T58 (a and b) S—CH₃ —CH₃ —CH₃  T59 (a and b) S —CH₃ —H —H  T60 (a and b) S —CH₃ —H —Cl T61 (a and b) S —CH₃ —H —Br  T62 (a and b) S —CH₃ —H —F  T63 (a and b)S —CH₃ —H —CH₃  T64 (a and b) S —CH₃ —H —CF₃  T65 (a and b) S —CH₃ —H—OCH₃  T66 (a and b) S —CH₃ —H —OCH₂CH₃  T67 (a and b) S —CH₃ —H —OCF₃ T68 (a and b) S —CH₃ —H -tert-butyl  T69 (a and b) S —CH₃ —H-iso-propyl  T70 (a and b) S —CF₃ —Cl —H  T71 (a and b) S —CF₃ —Br —H T72 (a and b) S —CF₃ —F —H  T73 (a and b) S —CF₃ —CH₃ —H  T74 (a and b)S —CF₃ —CF₃ —H  T75 (a and b) S —CF₃ —OCH₃ —H  T76 (a and b) S —CF₃—OCH₂CH₃ —H  T77 (a and b) S —CF₃ —OCF₃ —H  T78 (a and b) S —CF₃-tert-butyl —H  T79 (a and b) S —CF₃ -iso-propyl —H  T80 (a and b) S—CF₃ —CH₃ —CH₃  T81 (a and b) S —CF₃ —H —H  T82 (a and b) S —CF₃ —H —Cl T83 (a and b) S —CF₃ —H —Br  T84 (a and b) S —CF₃ —H —F  T85 (a and b)S —CF₃ —H —CH₃  T86 (a and b) S —CF₃ —H —CF₃  T87 (a and b) S —CF₃ —H—OCH₃  T88 (a and b) S —CF₃ —H —OCH₂CH₃  T89 (a and b) S —CF₃ —H —OCF₃ T90 (a and b) S —CF₃ —H -tert-butyl  T91 (a and b) S —CF₃ —H-iso-propyl  T92 (a and b) S —CHF₂ —Cl —H  T93 (a and b) S —CHF₂ —Br —H T94 (a and b) S —CHF₂ —F —H  T95 (a and b) S —CHF₂ —CH₃ —H  T96 (a andb) S —CHF₂ —CF₃ —H  T97 (a and b) S —CHF₂ —OCH₃ —H  T98 (a and b) S—CHF₂ —OCH₂CH₃ —H  T99 (a and b) S —CHF₂ —OCF₃ —H T100 (a and b) S —CHF₂-tert-butyl —H T101 (a and b) S —CHF₂ -iso-propyl —H T102 (a and b) S—CHF₂ —CH₃ —CH₃ T103 (a and b) S —CHF₂ —H —H T104 (a and b) S —CHF₂ —H—Cl T105 (a and b) S —CHF₂ —H —Br T106 (a and b) S —CHF₂ —H —F T107 (aand b) S —CHF₂ —H —CH₃ T108 (a and b) S —CHF₂ —H —CF₃ T109 (a and b) S—CHF₂ —H —OCH₃ T110 (a and b) S —CHF₂ —H —OCH₂CH₃ T111 (a and b) S —CHF₂—H —OCF₃ T112 (a and b) S —CHF₂ —H -tert-butyl T113 (a and b) S —CHF₂ —H-iso-propyl T114 (a and b) S —OH —Cl —H T115 (a and b) S —OH —Br —H T116(a and b) S —OH —F —H T117 (a and b) S —OH —CH₃ —H T118 (a and b) S —OH—CF₃ —H T119 (a and b) S —OH —OCH₃ —H T120 (a and b) S —OH —OCH₂CH₃ —HT121 (a and b) S —OH —OCF₃ —H T122 (a and b) S —OH -tert-butyl —H T123(a and b) S —OH -iso-propyl —H T124 (a and b) S —OH —CH₃ —CH₃ T125 (aand b) S —OH —H —H T126 (a and b) S —OH —H —Cl T127 (a and b) S —OH —H—Br T128 (a and b) S —OH —H —F T129 (a and b) S —OH —H —CH₃ T130 (a andb) S —OH —H —CF₃ T131 (a and b) S —OH —H —OCH₃ T132 (a and b) S —OH —H—OCH₂CH₃ T133 (a and b) S —OH —H —OCF₃ T134 (a and b) S —OH —H-tert-butyl T135 (a and b) S —OH —H -iso-propyl T136 (a and b) S —NO₂—Cl —H T137 (a and b) S —NO₂ —Br —H T138 (a and b) S —NO₂ —F —H T139 (aand b) S —NO₂ —CH₃ —H T140 (a and b) S —NO₂ —CF₃ —H T141 (a and b) S—NO₂ —OCH₃ —H T142 (a and b) S —NO₂ —OCH₂CH₃ —H T143 (a and b) S —NO₂—OCF₃ —H T144 (a and b) S —NO₂ -tert-butyl —H T145 (a and b) S —NO₂-iso-propyl —H T146 (a and b) S —NO₂ —CH₃ —CH₃ T147 (a and b) S —NO₂ —H—H T148 (a and b) S —NO₂ —H —Cl T149 (a and b) S —NO₂ —H —Br T150 (a andb) S —NO₂ —H —F T151 (a and b) S —NO₂ —H —CH₃ T152 (a and b) S —NO₂ —H—CF₃ T153 (a and b) S —NO₂ —H —OCH₃ T154 (a and b) S —NO₂ —H —OCH₂CH₃T155 (a and b) S —NO₂ —H —OCF₃ T156 (a and b) S —NO₂ —H -tert-butyl T157(a and b) S —NO₂ —H -iso-propyl T158 (a and b) S —CN —Br —H T159 (a andb) S —CN —Cl —H T160 (a and b) S —CN —F —H T161 (a and b) S —CN —CH₃ —HT162 (a and b) S —CN —CF₃ —H T163 (a and b) S —CN —OCH₃ —H T164 (a andb) S —CN —OCH₂CH₃ —H T165 (a and b) S —CN —OCF₃ —H T166 (a and b) S —CN-tert-butyl —H T167 (a and b) S —CN -iso-propyl —H T168 (a and b) S —CN—CH₃ —CH₃ T169 (a and b) S —CN —H —H T170 (a and b) S —CN —H —Cl T171 (aand b) S —CN —H —Br T172 (a and b) S —CN —H —F T173 (a and b) S —CN —H—CH₃ T174 (a and b) S —CN —H —CF₃ T175 (a and b) S —CN —H —OCH₃ T176 (aand b) S —CN —H —OCH₂CH₃ T177 (a and b) S —CN —H —OCF₃ T178 (a and b) S—CN —H -tert-butyl T179 (a and b) S —CN —H -iso-propyl T180 (a and b) S—Br —Br —H T181 (a and b) S —Br —Cl —H T182 (a and b) S —Br —F —H T183(a and b) S —Br —CH₃ —H T184 (a and b) S —Br —CF₃ —H T185 (a and b) S—Br —OCH₃ —H T186 (a and b) S —Br —OCH₂CH₃ —H T187 (a and b) S —Br —OCF₃—H T188 (a and b) S —Br -tert-butyl —H T189 (a and b) S —Br -iso-propyl—H T190 (a and b) S —Br —CH₃ —CH₃ T191 (a and b) S —Br —H —H T192 (a andb) S —Br —H —Cl T193 (a and b) S —Br —H —Br T194 (a and b) S —Br —H —FT195 (a and b) S —Br —H —CH₃ TI96 (a and b) S —Br —H —CF₃ T197 (a and b)S —Br —H —OCH₃ TI98 (a and b) S —Br —H —OCH₂CH₃ T199 (a and b) S —Br —H—OCF₃ T200 (a and b) S —Br —H -tert-butyl T201 (a and b) S —Br —H-iso-propyl T202 (a and b) S —I —Cl —H T203 (a and b) S —I —Br —H T204(a and b) S —I —F —H T205 (a and b) S —I —CH₃ —H T206 (a and b) S —I—CF₃ —H T207 (a and b) S —I —OCH₃ —H T208 (a and b) S —I —OCH₂CH₃ —HT209 (a and b) S —I —OCF₃ —H T210 (a and b) S —I -tert-butyl —H T211 (aand b) S —I -iso-propyl —H T212 (a and b) S —I —CH₃ —CH₃ T213 (a and b)S —I —H —H T214 (a and b) S —I —H —Cl T215 (a and b) S —I —H —Br T216 (aand b) S —I —H —F T217 (a and b) S —I —H —CH₃ T218 (a and b) S —I —H—CF₃ T219 (a and b) S —I —H —OCH₃ T220 (a and b) S —I —H —OCH₂CH₃ T221(a and b) S —I —H —OCF₃ T222 (a and b) S —I —H -tert-butyl T223 (a andb) S —I —H -iso-propyl T224 (a and b) O —H —Cl —H T225 (a and b) O —H—Br —H T226 (a and b) O —H —F —H T227 (a and b) O —H —CH₃ —H T228 (a andb) O —H —CF₃ —H T229 (a and b) O —H —OCH₃ —H T230 (a and b) O —H—OCH₂CH₃ —H T231 (a and b) O —H —OCF₃ —H T232 (a and b) O —H -tert-butyl—H T233 (a and b) O —H -iso-propyl —H T234 (a and b) O —H —CH₃ —CH₃ T235(a and b) O —H —H —H T236 (a and b) O —H —H —Cl T237 (a and b) O —H —H—Br T238 (a and b) O —H —H —F T239 (a and b) O —H —H —CH₃ T240 (a and b)O —H —H —CF₃ T241 (a and b) O —H —H —OCH₃ T242 (a and b) O —H —H—OCH₂CH₃ T243 (a and b) O —H —H —OCF₃ T244 (a and b) O —H —H -tert-butylT245 (a and b) O —H —H -iso-propyl T246 (a and b) O —Cl —Cl —H T247 (aand b) O —Cl —Br —H T248 (a and b) O —Cl —F —H T249 (a and b) O —Cl —CH₃—H T250 (a and b) O —Cl —CF₃ —H T251 (a and b) O —Cl —OCH₃ —H T252 (aand b) O —Cl —OCH₂CH₃ —H T253 (a and b) O —Cl —OCF₃ —H T254 (a and b) O—Cl -tert-butyl —H T255 (a and b) O —Cl -iso-propyl —H T256 (a and b) O—Cl —CH₃ —CH₃ T257 (a and b) O —Cl —H —H T258 (a and b) O —Cl —H —CH₃T259 (a and b) O —Cl —H —Cl T260 (a and b) O —Cl —H —Br T261 (a and b) O—Cl —H —F T262 (a and b) O —Cl —H —CF₃ T263 (a and b) O —Cl —H —OCH₃T264 (a and b) O —Cl —H —OCH₂CH₃ T265 (a and b) O —Cl —H —OCF₃ T266 (aand b) O —Cl —H -tert-butyl T267 (a and b) O —Cl —H -iso-propyl T268 (aand b) O —Cl —H —OCF₃ T269 (a and b) O —Cl —H -tert-butyl T270 (a and b)O —Cl —H -iso-propyl T271 (a and b) O —CH₃ —Cl —H T272 (a and b) O —CH₃—Br —H T273 (a and b) O —CH₃ —F —H T274 (a and b) O —CH₃ —CH₃ —H T275 (aand b) O —CH₃ —CF₃ —H T276 (a and b) O —CH₃ —OCH₃ —H T277 (a and b) O—CH₃ —OCH₂CH₃ —H T278 (a and b) O —CH₃ —OCF₃ —H T279 (a and b) O —CH₃-tert-butyl —H T280 (a and b) O —CH₃ -iso-propyl —H T281 (a and b) O—CH₃ —CH₃ —CH₃ T282 (a and b) O —CH₃ —H —H T283 (a and b) O —CH₃ —H —ClT284 (a and b) O —CH₃ —H —Br T285 (a and b) O —CH₃ —H —F T286 (a and b)O —CH₃ —H —CH₃ T287 (a and b) O —CH₃ —H —CF₃ T288 (a and b) O —CH₃ —H—OCH₃ T289 (a and b) O —CH₃ —H —OCH₂CH₃ T290 (a and b) O —CH₃ —H —OCF₃T291 (a and b) O —CH₃ —H -tert-butyl T292 (a and b) O —CH₃ —H-iso-propyl T293 (a and b) O —CF₃ —Cl —H T294 (a and b) O —CF₃ —Br —HT295 (a and b) O —CF₃ —F —H T296 (a and b) O —CF₃ —CH₃ —H T297 (a and b)O —CF₃ —CF₃ —H T298 (a and b) O —CF₃ —OCH₃ —H T299 (a and b) O —CF₃—OCH₂CH₃ —H T300 (a and b) O —CF₃ —OCF₃ —H T301 (a and b) O —CF₃-tert-butyl —H T302 (a and b) O —CF₃ -iso-propyl —H T303 (a and b) O—CF₃ —CH₃ —CH₃ T304 (a and b) O —CF₃ —H —H T305 (a and b) O —CF₃ —H —ClT306 (a and b) O —CF₃ —H —Br T307 (a and b) O —CF₃ —H —F T308 (a and b)O —CF₃ —H —CH₃ T309 (a and b) O —CF₃ —H —CF₃ T310 (a and b) O —CF₃ —H—OCH₃ T311 (a and b) O —CF₃ —H —OCH₂CH₃ T312 (a and b) O —CF₃ —H —OCF₃T313 (a and b) O —CF₃ —H -tert-butyl T314 (a and b) O —CF₃ —H-iso-propyl T315 (a and b) O —CHF₂ —Cl —H T316 (a and b) O —CHF₂ —Br —HT317 (a and b) O —CHF₂ —F —H T318 (a and b) O —CHF₂ —CH₃ —H T319 (a andb) O —CHF₂ —CF₃ —H T320 (a and b) O —CHF₂ —OCH₃ —H T321 (a and b) O—CHF₂ —OCH₂CH₃ —H T322 (a and b) O —CHF₂ —OCF₃ —H T323 (a and b) O —CHF₂-tert-butyl —H T324 (a and b) O —CHF₂ -iso-propyl —H T325 (a and b) O—CHF₂ —CH₃ —CH₃ T326 (a and b) O —CHF₂ —H —H T327 (a and b) O —CHF₂ —H—Cl T328 (a and b) O —CHF₂ —H —Br T329 (a and b) O —CHF₂ —H —F T330 (aand b) O —CHF₂ —H —CH₃ T331 (a and b) O —CHF₂ —H —CF₃ T332 (a and b) O—CHF₂ —H —OCH₃ T333 (a and b) O —CHF₂ —H —OCH₂CH₃ T334 (a and b) O —CHF₂—H —OCF₃ T335 (a and b) O —CHF₂ —H -tert-butyl T336 (a and b) O —CHF₂ —H-iso-propyl T337 (a and b) O —OH —Cl —H T338 (a and b) O —OH —Br —H T339(a and b) O —OH —F —H T340 (a and b) O —OH —CH₃ —H T341 (a and b) O —OH—CF₃ —H T342 (a and b) O —OH —OCH₃ —H T343 (a and b) O —OH —OCH₂CH₃ —HT344 (a and b) O —OH —OCF₃ —H T345 (a and b) O —OH -tert-butyl —H T346(a and b) O —OH -iso-propyl —H T347 (a and b) O —OH —CH₃ —CH₃ T348 (aand b) O —OH —H —H T349 (a and b) O —OH —H —Cl T350 (a and b) O —OH —H—Br T351 (a and b) O —OH —H —F T352 (a and b) O —OH —H —CH₃ T353 (a andb) O —OH —H —CF₃ T354 (a and b) O —OH —H —OCH₃ T355 (a and b) O —OH —H—OCH₂CH₃ T356 (a and b) O —OH —H —OCF₃ T357 (a and b) O —OH —H-tert-butyl T358 (a and b) O —OH —H -iso-propyl T359 (a and b) O —NO₂—Cl —H T360 (a and b) O —NO₂ —Br —H T361 (a and b) O —NO₂ —F —H T362 (aand b) O —NO₂ —CH₃ —H T363 (a and b) O —NO₂ —CF₃ —H T364 (a and b) O—NO₂ —OCH₃ —H T365 (a and b) O —NO₂ —OCH₂CH₃ —H T366 (a and b) O —NO₂—OCF₃ —H T367 (a and b) O —NO₂ -tert-butyl —H T368 (a and b) O —NO₂-iso-propyl —H T369 (a and b) O —NO₂ —CH₃ —CH₃ T370 (a and b) O —NO₂ —H—H T371 (a and b) O —NO₂ —H —Cl T372 (a and b) O —NO₂ —H —Br T373 (a andb) O —NO₂ —H —F T374 (a and b) O —NO₂ —H —CH₃ T375 (a and b) O —NO₂ —H—CF₃ T376 (a and b) O —NO₂ —H —OCH₃ T377 (a and b) O —NO₂ —H —OCH₂CH₃T378 (a and b) O —NO₂ —H —OCF₃ T379 (a and b) O —NO₂ —H -tert-butyl T380(a and b) O —NO₂ —H -iso-propyl T381 (a and b) O —CN —Br —H T382 (a andb) O —CN —Cl —H T383 (a and b) O —CN —F —H T384 (a and b) O —CN —CH₃ —HT385 (a and b) O —CN —CF₃ —H T386 (a and b) O —CN —OCH₃ —H T387 (a andb) O —CN —OCH₂CH₃ —H T388 (a and b) O —CN —OCF₃ —H T389 (a and b) O —CN-tert-butyl —H T390 (a and b) O —CN -iso-propyl —H T391 (a and b) O —CN—CH₃ —CH₃ T392 (a and b) O —CN —H —H T393 (a and b) O —CN —H —Cl T394 (aand b) O —CN —H —Br T395 (a and b) O —CN —H —F T396 (a and b) O —CN —H—CH₃ T397 (a and b) O —CN —H —CF₃ T398 (a and b) O —CN —H —OCH₃ T399 (aand b) O —CN —H —OCH₂CH₃ T400 (a and b) O —CN —H —OCF₃ T401 (a and b) O—CN —H -tert-butyl T402 (a and b) O —CN —H -iso-propyl T403 (a and b) O—Br —Br —H T404 (a and b) O —Br —Cl —H T405 (a and b) O —Br —F —H T406(a and b) O —Br —CH₃ —H T407 (a and b) O —Br —CF₃ —H T408 (a and b) O—Br —OCH₃ —H T409 (a and b) O —Br —OCH₂CH₃ —H T410 (a and b) O —Br —OCF₃—H T411 (a and b) O —Br -tert-butyl —H T412 (a and b) O —Br -iso-propyl—H T413 (a and b) O —Br —CH₃ —CH₃ T414 (a and b) O —Br —H —H T415 (a andb) O —Br —H —Cl T416 (a and b) O —Br —H —Br T417 (a and b) O —Br —H —FT418 (a and b) O —Br —H —CH₃ T419 (a and b) O —Br —H —CF₃ T420 (a and b)O —Br —H —OCH₃ T421 (a and b) O —Br —H —OCH₂CH₃ T422 (a and b) O —Br —H—OCF₃ T423 (a and b) O —Br —H -tert-butyl T424 (a and b) O —Br —H-iso-propyl T425 (a and b) O —I —Cl —H T426 (a and b) O —I —Br —H T427(a and b) O —I —F —H T428 (a and b) O —I —CH₃ —H T429 (a and b) O —I—CF₃ —H T430 (a and b) O —I —OCH₃ —H T431 (a and b) O —I —OCH₂CH₃ —HT432 (a and b) O —I —OCF₃ —H T433 (a and b) O —I -tert-butyl —H T434 (aand b) O —I -iso-propyl —H T435 (a and b) O —I —CH₃ —CH₃ T436 (a and b)O —I —H —H T437 (a and b) O —I —H —Cl T438 (a and b) O —I —H —Br T439 (aand b) O —I —H —F T440 (a and b) O —I —H —CH₃ T441 (a and b) O —I —H—CF₃ T442 (a and b) O —I —H —OCH₃ T443 (a and b) O —I —H —OCH₂CH₃ T444(a and b) O —I —H —OCF₃ T445 (a and b) O —I —H -tert-butyl T446 (a andb) O —I —H -iso-propyl T447 (a and b) NH —H —Cl —H T448 (a and b) NH —H—Br —H T449 (a and b) NH —H —F —H T450 (a and b) NH —H —CH₃ —H T451 (aand b) NH —H —CF₃ —H T452 (a and b) NH —H —OCH₃ —H T453 (a and b) NH —H—OCH₂CH₃ —H T454 (a and b) NH —H —OCF₃ —H T455 (a and b) NH —H-tert-butyl —H T456 (a and b) NH —H -iso-propyl —H T457 (a and b) NH —H—CH₃ —CH₃ T458 (a and b) NH —H —H —H T459 (a and b) NH —H —H —Cl T460 (aand b) NH —H —H —Br T461 (a and b) NH —H —H —F T462 (a and b) NH —H —H—CH₃ T463 (a and b) NH —H —H —CF₃ T464 (a and b) NH —H —H —OCH₃ T465 (aand b) NH —H —H —OCH₂CH₃ T466 (a and b) NH —H —H —OCF₃ T467 (a and b) NH—H —H -tert-butyl T468 (a and b) NH —H —H -iso-propyl T469 (a and b) NH—Cl —Cl —H T470 (a and b) NH —Cl —Br —H T471 (a and b) NH —Cl —F —H T472(a and b) NH —Cl —CH₃ —H T473 (a and b) NH —Cl —CF₃ —H T474 (a and b) NH—Cl —OCH₃ —H T475 (a and b) NH —Cl —OCH₂CH₃ —H T476 (a and b) NH —Cl—OCF₃ —H T477 (a and b) NH —Cl -tert-butyl —H T478 (a and b) NH —Cl-iso-propyl —H T479 (a and b) NH —Cl —CH₃ —CH₃ T480 (a and b) NH —Cl —H—H T481 (a and b) NH —Cl —H —CH₃ T482 (a and b) NH —Cl —H —Cl T483 (aand b) NH —Cl —H —Br T484 (a and b) NH —Cl —H —F T485 (a and b) NH —Cl—H —CF₃ T486 (a and b) NH —Cl —H —OCH₃ T487 (a and b) NH —Cl —H —OCH₂CH₃T488 (a and b) NH —Cl —H —OCF₃ T489 (a and b) NH —Cl —H -tert-butyl T490(a and b) NH —Cl —H -iso-propyl T491 (a and b) NH —Cl —H —OCF₃ T492 (aand b) NH —Cl —H -tert-butyl T493 (a and b) NH —Cl —H -iso-propyl T494(a and b) NH —CH₃ —Cl —H T495 (a and b) NH —CH₃ —Br —H T496 (a and b) NH—CH₃ —F —H T497 (a and b) NH —CH₃ —CH₃ —H T498 (a and b) NH —CH₃ —CF₃ —HT499 (a and b) NH —CH₃ —OCH₃ —H T500 (a and b) NH —CH₃ —OCH₂CH₃ —H T501(a and b) NH —CH₃ —OCF₃ —H T502 (a and b) NH —CH₃ -tert-butyl —H T503 (aand b) NH —CH₃ -iso-propyl —H T504 (a and b) NH —CH₃ —CH₃ —CH₃ T505 (aand b) NH —CH₃ —H —H T506 (a and b) NH —CH₃ —H —Cl T507 (a and b) NH—CH₃ —H —Br T508 (a and b) NH —CH₃ —H —F T509 (a and b) NH —CH₃ —H —CH₃T510 (a and b) NH —CH₃ —H —CF₃ T511 (a and b) NH —CH₃ —H —OCH₃ T512 (aand b) NH —CH₃ —H —OCH₂CH₃ T513 (a and b) NH —CH₃ —H —OCF₃ T514 (a andb) NH —CH₃ —H -tert-butyl T515 (a and b) NH —CH₃ —H -iso-propyl T516 (aand b) NH —CF₃ —Cl —H T517 (a and b) NH —CF₃ —Br —H T518 (a and b) NH—CF₃ —F —H T519 (a and b) NH —CF₃ —CH₃ —H T520 (a and b) NH —CF₃ —CF₃ —HT521 (a and b) NH —CF₃ —OCH₃ —H T522 (a and b) NH —CF₃ —OCH₂CH₃ —H T523(a and b) NH —CF₃ —OCF₃ —H T524 (a and b) NH —CF₃ -tert-butyl —H T525 (aand b) NH —CF₃ -iso-propyl —H T526 (a and b) NH —CF₃ —CH₃ —CH₃ T527 (aand b) NH —CF₃ —H —H T528 (a and b) NH —CF₃ —H —Cl T529 (a and b) NH—CF₃ —H —Br T530 (a and b) NH —CF₃ —H —F T531 (a and b) NH —CF₃ —H —CH₃T532 (a and b) NH —CF₃ —H —CF₃ T533 (a and b) NH —CF₃ —H —OCH₃ T534 (aand b) NH —CF₃ —H —OCH₂CH₃ T535 (a and b) NH —CF₃ —H —OCF₃ T536 (a andb) NH —CF₃ —H -tert-butyl T537 (a and b) NH —CF₃ —H -iso-propyl T538 (aand b) NH —CHF₂ —Cl —H T539 (a and b) NH —CHF₂ —Br —H T540 (a and b) NH—CHF₂ —F —H T541 (a and b) NH —CHF₂ —CH₃ —H T542 (a and b) NH —CHF₂ —CF₃—H T543 (a and b) NH —CHF₂ —OCH₃ —H T544 (a and b) NH —CHF₂ —OCH₂CH₃ —HT545 (a and b) NH —CHF₂ —OCF₃ —H T546 (a and b) NH —CHF₂ -tert-butyl —HT547 (a and b) NH —CHF₂ -iso-propyl —H T548 (a and b) NH —CHF₂ —CH₃ —CH₃T549 (a and b) NH —CHF₂ —H —H T550 (a and b) NH —CHF₂ —H —Cl T551 (a andb) NH —CHF₂ —H —Br T552 (a and b) NH —CHF₂ —H —F T553 (a and b) NH —CHF₂—H —CH₃ T554 (a and b) NH —CHF₂ —H —CF₃ T555 (a and b) NH —CHF₂ —H —OCH₃T556 (a and b) NH —CHF₂ —H —OCH₂CH₃ T557 (a and b) NH —CHF₂ —H —OCF₃T558 (a and b) NH —CHF₂ —H -tert-butyl T559 (a and b) NH —CHF₂ —H-iso-propyl T560 (a and b) NH —OH —Cl —H T561 (a and b) NH —OH —Br —HT562 (a and b) NH —OH —F —H T563 (a and b) NH —OH —CH₃ —H T564 (a and b)NH —OH —CF₃ —H T565 (a and b) NH —OH —OCH₃ —H T566 (a and b) NH —OH—OCH₂CH₃ —H T567 (a and b) NH —OH —OCF₃ —H T568 (a and b) NH —OH-tert-butyl —H T569 (a and b) NH —OH -iso-propyl —H T570 (a and b) NH—OH —CH₃ —CH₃ T571 (a and b) NH —OH —H —H T572 (a and b) NH —OH —H —ClT573 (a and b) NH —OH —H —Br T574 (a and b) NH —OH —H —F T575 (a and b)NH —OH —H —CH₃ T576 (a and b) NH —OH —H —CF₃ T577 (a and b) NH —OH —H—OCH₃ T578 (a and b) NH —OH —H —OCH₂CH₃ T579 (a and b) NH —OH —H —OCF₃T580 (a and b) NH —OH —H -tert-butyl T581 (a and b) NH —OH —H-iso-propyl T582 (a and b) NH —NO₂ —Cl —H T583 (a and b) NH —NO₂ —Br —HT584 (a and b) NH —NO₂ —F —H T585 (a and b) NH —NO₂ —CH₃ —H T586 (a andb) NH —NO₂ —CF₃ —H T587 (a and b) NH —NO₂ —OCH₃ —H T588 (a and b) NH—NO₂ —OCH₂CH₃ —H T589 (a and b) NH —NO₂ —OCF₃ —H T590 (a and b) NH —NO₂-tert-butyl —H T591 (a and b) NH —NO₂ -iso-propyl —H T592 (a and b) NH—NO₂ —CH₃ —CH₃ T593 (a and b) NH —NO₂ —H —H T594 (a and b) NH —NO₂ —H—Cl T595 (a and b) NH —NO₂ —H —Br T596 (a and b) NH —NO₂ —H —F T597 (aand b) NH —NO₂ —H —CH₃ T598 (a and b) NH —NO₂ —H —CF₃ T599 (a and b) NH—NO₂ —H —OCH₃ T600 (a and b) NH —NO₂ —H —OCH₂CH₃ T601 (a and b) NH —NO₂—H —OCF₃ T602 (a and b) NH —NO₂ —H -tert-butyl T603 (a and b) NH —NO₂ —H-iso-propyl T604 (a and b) NH —CN —Br —H T605 (a and b) NH —CN —Cl —HT606 (a and b) NH —CN —F —H T607 (a and b) NH —CN —CH₃ —H T608 (a and b)NH —CN —CF₃ —H T609 (a and b) NH —CN —OCH₃ —H T610 (a and b) NH —CN—OCH₂CH₃ —H T611 (a and b) NH —CN —OCF₃ —H T612 (a and b) NH —CN-tert-butyl —H T613 (a and b) NH —CN -iso-propyl —H T614 (a and b) NH—CN —CH₃ —CH₃ T615 (a and b) NH —CN —H —H T616 (a and b) NH —CN —H —ClT617 (a and b) NH —CN —H —Br T618 (a and b) NH —CN —H —F T619 (a and b)NH —CN —H —CH₃ T620 (a and b) NH —CN —H —CF₃ T621 (a and b) NH —CN —H—OCH₃ T622 (a and b) NH —CN —H —OCH₂CH₃ T623 (a and b) NH —CN —H —OCF₃T624 (a and b) NH —CN —H -tert-butyl T625 (a and b) NH —CN —H-iso-propyl T626 (a and b) NH —Br —Br —H T627 (a and b) NH —Br —Cl —HT628 (a and b) NH —Br —F —H T629 (a and b) NH —Br —CH₃ —H T630 (a and b)NH —Br —CF₃ —H T631 (a and b) NH —Br —OCH₃ —H T632 (a and b) NH —Br—OCH₂CH₃ —H T633 (a and b) NH —Br —OCF₃ —H T634 (a and b) NH —Br-tert-butyl —H T635 (a and b) NH —Br -iso-propyl —H T636 (a and b) NH—Br —CH₃ —CH₃ T637 (a and b) NH —Br —H —H T638 (a and b) NH —Br —H —ClT639 (a and b) NH —Br —H —Br T640 (a and b) NH —Br —H —F T641 (a and b)NH —Br —H —CH₃ T642 (a and b) NH —Br —H —CF₃ T643 (a and b) NH —Br —H—OCH₃ T644 (a and b) NH —Br —H —OCH₂CH₃ T645 (a and b) NH —Br —H —OCF₃T646 (a and b) NH —Br —H -tert-butyl T647 (a and b) NH —Br —H-iso-propyl T648 (a and b) NH —I —Cl —H T649 (a and b) NH —I —Br —H T650(a and b) NH —I —F —H T651 (a and b) NH —I —CH₃ —H T652 (a and b) NH —I—CF₃ —H T653 (a and b) NH —I —OCH₃ —H T654 (a and b) NH —I —OCH₂CH₃ —HT655 (a and b) NH —I —OCF₃ —H T656 (a and b) NH —I -tert-butyl —H T657(a and b) NH —I -iso-propyl —H T658 (a and b) NH —I —CH₃ —CH₃ T659 (aand b) NH —I —H —H T660 (a and b) NH —I —H —Cl T661 (a and b) NH —I —H—Br T662 (a and b) NH —I —H —F T663 (a and b) NH —I —H —CH₃ T664 (a andb) NH —I —H —CF₃ T665 (a and b) NH —I —H —OCH₃ T666 (a and b) NH —I —H—OCH₂CH₃ T667 (a and b) NH —I —H —OCF₃ T668 (a and b) NH —I —H-tert-butyl T669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 21 (Iu)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  U1 (a and b) —H —H  U2 (a and b) —H -tert-butyl  U3 (a and b) —H-iso-butyl  U4 (a and b) —H -sec-butyl  U5 (a and b) —H -iso-propyl  U6(a and b) —H -n-propyl  U7 (a and b) —H -cyclohexyl  U8 (a and b) —H-tert-butoxy  U9 (a and b) —H -isopropoxy  U10 (a and b) —H —CF₃  U11 (aand b) —H —CH₂CF₃  U12 (a and b) —H —OCF₃  U13 (a and b) —H —Cl  U14 (aand b) —H —Br  U15 (a and b) —H —I  U16 (a and b) —H -n-butyl  U17 (aand b) —H —CH₃  U18 (a and b) —H —SCF₃  U19 (a and b) —H —N(CH₂CH₃)₂ U20 (a and b) —H —OCF₂CHF₂  U21 (a and b) —H —C(OH)(CF₃)₂  U22 (a andb) —H -(1,1-dimethyl-pentyl)  U23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester  U24 (a and b) —H —N-piperidinyl  U25 (a and b) —Cl —H U26 (a and b) —Cl -tert-butyl  U27 (a and b) —Cl -iso-butyl  U28 (a andb) —Cl -sec-butyl  U29 (a and b) —Cl -iso-propyl  U30 (a and b) —Cl-n-propyl  U31 (a and b) —Cl -cyclohexyl  U32 (a and b) —Cl -tert-butoxy U33 (a and b) —Cl -isopropoxy  U34 (a and b) —Cl —CF₃  U35 (a and b)—Cl —CH₂CF₃  U36 (a and b) —Cl —OCF₃  U37 (a and b) —Cl —Cl  U38 (a andb) —Cl —Br  U39 (a and b) —Cl —I  U40 (a and b) —Cl -n-butyl  U41 (a andb) —Cl —CH₃  U42 (a and b) —Cl —SCF₃  U43 (a and b) —Cl —N(CH₂CH₃)₂  U44(a and b) —Cl —OCF₂CHF₂  U45 (a and b) —Cl —C(OH)(CF₃)₂  U46 (a and b)—Cl -(1,1-dimethyl-pentyl)  U47 (a and b) —Cl (1,1-dimethyl-acetic acid)ethyl ester  U48 (a and b) —Cl —N-piperidinyl  U49 (a and b) —F —H  U50(a and b) —F -tert-butyl  U51 (a and b) —F -iso-butyl  U52 (a and b) —F-sec-butyl  U53 (a and b) —F -iso-propyl  U54 (a and b) —F -n-propyl U55 (a and b) —F -cyclohexyl  U56 (a and b) —F -tert-butoxy  U57 (a andb) —F -isopropoxy  U58 (a and b) —F —CF₃  U59 (a and b) —F —CH₂CF₃  U60(a and b) —F —OCF₃  U61 (a and b) —F —Cl  U62 (a and b) —F —Br  U63 (aand b) —F —I  U64 (a and b) —F -n-butyl  U65 (a and b) —F —CH₃  U66 (aand b) —F —SCF₃  U67 (a and b) —F —N(CH₂CH₃)₂  U68 (a and b) —F—OCF₂CHF₂  U69 (a and b) —F —C(OH)(CF₃)₂  U70 (a and b) —F-(1,1-dimethyl-pentyl)  U71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester  U72 (a and b) —F —N-piperidinyl  U73 (a and b) —CH₃ —H  U74(a and b) —CH₃ -iso-butyl  U75 (a and b) —CH₃ -tert-butyl  U76 (a and b)—CH₃ -sec-butyl  U77 (a and b) —CH₃ -iso-propyl  U78 (a and b) —CH₃-n-propyl  U79 (a and b) —CH₃ -cyclohexyl  U80 (a and b) —CH₃-tert-butoxy  U81 (a and b) —CH₃ -isopropoxy  U82 (a and b) —CH₃ —CF₃ U83 (a and b) —CH₃ —CH₂CF₃  U84 (a and b) —CH₃ —OCF₃  U85 (a and b)—CH₃ —Cl  U86 (a and b) —CH₃ —Br  U87 (a and b) —CH₃ —I  U88 (a and b)—CH₃ -n-butyl  U89 (a and b) —CH₃ —CH₃  U90 (a and b) —CH₃ —SCF₃  U91 (aand b) —CH₃ —N(CH₂CH₃)₂  U92 (a and b) —CH₃ —OCF₂CHF₂  U93 (a and b)—CH₃ —C(OH)(CF₃)₂  U94 (a and b) —CH₃ -(1,1-dimethyl-pentyl)  U95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester  U96 (a and b) —CH₃—N-piperidinyl  U97 (a and b) —CF₃ —H  U98 (a and b) —CF₃ -tert-butyl U99 (a and b) —CF₃ -iso-butyl U100 (a and b) —CF₃ -sec-butyl U101 (aand b) —CF₃ -iso-propyl U102 (a and b) —CF₃ -n-propyl U103 (a and b)—CF₃ -cyclohexyl U104 (a and b) —CF₃ -tert-butoxy U105 (a and b) —CF₃-isopropoxy U106 (a and b) —CF₃ —CF₃ U107 (a and b) —CF₃ —CH₂CF₃ U108 (aand b) —CF₃ —OCF₃ U109 (a and b) —CF₃ —Cl U110 (a and b) —CF₃ —Br U111(a and b) —CF₃ —I U112 (a and b) —CF₃ -n-butyl U113 (a and b) —CF₃ —CH₃U114 (a and b) —CF₃ —SCF₃ U115 (a and b) —CF₃ —N(CH₂CH₃)₂ U116 (a and b)—CF₃ —OCF₂CHF₂ U117 (a and b) —CF₃ —C(OH)(CF₃)₂ U118 (a and b) —CF₃-(1,1-dimethyl-pentyl) U119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester U120 (a and b) —CF₃ —N-piperidinyl U121 (a and b) —CHF₂-tert-butyl U122 (a and b) —CHF₂ —H U123 (a and b) —CHF₂ -iso-butyl U124(a and b) —CHF₂ -sec-butyl U125 (a and b) —CHF₂ -iso-propyl U126 (a andb) —CHF₂ -n-propyl U127 (a and b) —CHF₂ -cyclohexyl U128 (a and b) —CHF₂-tert-butoxy U129 (a and b) —CHF₂ -isopropoxy U130 (a and b) —CHF₂ —CF₃U131 (a and b) —CHF₂ —CH₂CF₃ U132 (a and b) —CHF₂ —OCF₃ U133 (a and b)—CHF₂ —Cl U134 (a and b) —CHF₂ —Br U135 (a and b) —CHF₂ —I U136 (a andb) —CHF₂ -n-butyl U137 (a and b) —CHF₂ —CH₃ U138 (a and b) —CHF₂ —SCF₃U139 (a and b) —CHF₂ —N(CH₂CH₃)₂ U140 (a and b) —CHF₂ —OCF₂CHF₂ U141 (aand b) —CHF₂ —C(OH)(CF₃)₂ U142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)U143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester U144 (a andb) —CHF₂ —N-piperidinyl U145 (a and b) —OH —H U146 (a and b) —OH-tert-butyl U147 (a and b) —OH -iso-butyl U148 (a and b) —OH -sec-butylU149 (a and b) —OH -iso-propyl U150 (a and b) —OH -n-propyl U151 (a andb) —OH -cyclohexyl U152 (a and b) —OH -tert-butoxy U153 (a and b) —OH-isopropoxy U154 (a and b) —OH —CF₃ U155 (a and b) —OH —CH₂CF₃ U156 (aand b) —OH —OCF₃ U157 (a and b) —OH —Cl U158 (a and b) —OH —Br U159 (aand b) —OH —I U160 (a and b) —OH -n-butyl U161 (a and b) —OH —CH₃ U162(a and b) —OH —SCF₃ U163 (a and b) —OH —N(CH₂CH₃)₂ U164 (a and b) —OH—OCF₂CHF₂ U165 (a and b) —OH —C(OH)(CF₃)₂ U166 (a and b) —OH-(1,1-dimethyl-pentyl) U167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester U168 (a and b) —OH —N-piperidinyl U169 (a and b) —NO₂ —HU170 (a and b) —NO₂ -tert-butyl U171 (a and b) —NO₂ -iso-butyl U172 (aand b) —NO₂ -sec-butyl U173 (a and b) —NO₂ -iso-propyl U174 (a and b)—NO₂ -n-propyl U175 (a and b) —NO₂ -cyclohexyl U176 (a and b) —NO₂-tert-butoxy U177 (a and b) —NO₂ -isopropoxy U178 (a and b) —NO₂ —CF₃U179 (a and b) —NO₂ —CH₂CF₃ U180 (a and b) —NO₂ —OCF₃ U181 (a and b)—NO₂ —Cl U182 (a and b) —NO₂ —Br U183 (a and b) —NO₂ —I U184 (a and b)—NO₂ -n-butyl U185 (a and b) —NO₂ —CH₃ U186 (a and b) —NO₂ —SCF₃ U187 (aand b) —NO₂ —N(CH₂CH₃)₂ U188 (a and b) —NO₂ —OCF₂CHF₂ U189 (a and b)—NO₂ —C(OH)(CF₃)₂ U190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) U191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester U192 (a and b) —NO₂—N-piperidinyl U193 (a and b) —CN —H U194 (a and b) —CN -tert-butyl U195(a and b) —CN -iso-butyl U196 (a and b) —CN -sec-butyl U197 (a and b)—CN -iso-propyl U198 (a and b) —CN -n-propyl U199 (a and b) —CN-cyclohexyl U200 (a and b) —CN -tert-butoxy U201 (a and b) —CN-isopropoxy U202 (a and b) —CN —CF₃ U203 (a and b) —CN —CH₂CF₃ U204 (aand b) —CN —OCF₃ U205 (a and b) —CN —Cl U206 (a and b) —CN —Br U207 (aand b) —CN —I U208 (a and b) —CN -n-butyl U209 (a and b) —CN —CH₃ U210(a and b) —CN —SCF₃ U211 (a and b) —CN —N(CH₂CH₃)₂ U212 (a and b) —CN—OCF₂CHF₂ U213 (a and b) —CN —C(OH)(CF₃)₂ U214 (a and b) —CN-(1,1-dimethyl-pentyl) U215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester U216 (a and b) —CN —N-piperidinyl U217 (a and b) —Br —H U218(a and b) —Br -tert-butyl U219 (a and b) —Br -iso-butyl U220 (a and b)—Br -sec-butyl U221 (a and b) —Br -iso-propyl U222 (a and b) —Br-n-propyl U223 (a and b) —Br -cyclohexyl U224 (a and b) —Br -tert-butoxyU225 (a and b) —Br -isopropoxy U226 (a and b) —Br —CF₃ U227 (a and b)—Br —CH₂CF₃ U228 (a and b) —Br —OCF₃ U229 (a and b) —Br —Cl U230 (a andb) —Br —Br U231 (a and b) —Br —I U232 (a and b) —Br -n-butyl U233 (a andb) —Br —CH₃ U234 (a and b) —Br —SCF₃ U235 (a and b) —Br —N(CH₂CH₃)₂ U236(a and b) —Br —OCF₂CHF₂ U237 (a and b) —Br —C(OH)(CF₃)₂ U238 (a and b)—Br -(1,1-dimethyl-pentyl) U239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester U240 (a and b) —Br —N-piperidinyl U241 (a and b) —I-tert-butyl U242 (a and b) —I —H U243 (a and b) —I -iso-butyl U244 (aand b) —I -sec-butyl U245 (a and b) —I -iso-propyl U246 (a and b) —I-n-propyl U247 (a and b) —I -cyclohexyl U248 (a and b) —I -tert-butoxyU249 (a and b) —I -isopropoxy U250 (a and b) —I —CF₃ U251 (a and b) —I—CH₂CF₃ U252 (a and b) —I —OCF₃ U253 (a and b) —I —Cl U254 (a and b) —I—Br U255 (a and b) —I —I U256 (a and b) —I -n-butyl U257 (a and b) —I—CH₃ U258 (a and b) —I —SCF₃ U259 (a and b) —I —N(CH₂CH₃)₂ U260 (a andb) —I —OCF₂CHF₂ U261 (a and b) —I —C(OH)(CF₃)₂ U262 (a and b) —I-(1,1-dimethyl-pentyl) U263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester U264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R3 is —CH₃.

TABLE 22 (Iv)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  V1 (a and b) —H —H  V2 (a and b) —H -tert-butyl  V3 (a and b) —H-iso-butyl  V4 (a and b) —H -sec-butyl  V5 (a and b) —H -iso-propyl  V6(a and b) —H -n-propyl  V7 (a and b) —H -cyclohexyl  V8 (a and b) —H-tert-butoxy  V9 (a and b) —H -isopropoxy  V10 (a and b) —H —CF₃  V11 (aand b) —H —CH₂CF₃  V12 (a and b) —H —OCF₃  V13 (a and b) —H —Cl  V14 (aand b) —H —Br  V15 (a and b) —H —I  V16 (a and b) —H -n-butyl  V17 (aand b) —H —CH₃  V18 (a and b) —H —SCF₃  V19 (a and b) —H —N(CH₂CH₃)₂ V20 (a and b) —H —OCF₂CHF₂  V21 (a and b) —H —C(OH)(CF₃)₂  V22 (a andb) —H -(1,1-dimethyl-pentyl)  V23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester  V24 (a and b) —H —N-piperidinyl  V25 (a and b) —Cl —H V26 (a and b) —Cl -tert-butyl  V27 (a and b) —Cl -iso-butyl  V28 (a andb) —Cl -sec-butyl  V29 (a and b) —Cl -iso-propyl  V30 (a and b) —Cl-n-propyl  V31 (a and b) —Cl -cyclohexyl  V32 (a and b) —Cl -tert-butoxy V33 (a and b) —Cl -isopropoxy  V34 (a and b) —Cl —CF₃  V35 (a and b)—Cl —CH₂CF₃  V36 (a and b) —Cl —OCF₃  V37 (a and b) —Cl —Cl  V38 (a andb) —Cl —Br  V39 (a and b) —Cl —I  V40 (a and b) —Cl -n-butyl  V41 (a andb) —Cl —CH₃  V42 (a and b) —Cl —SCF₃  V43 (a and b) —Cl —N(CH₂CH₃)₂  V44(a and b) —Cl —OCF₂CHF₂  V45 (a and b) —Cl —C(OH)(CF₃)₂  V46 (a and b)—Cl -(1,1-dimethyl-pentyl)  V47 (a and b) —Cl -(1,1-dimethyl-aceticacid) ethyl ester  V48 (a and b) —Cl —N-piperidinyl  V49 (a and b) —F —H V50 (a and b) —F -tert-butyl  V51 (a and b) —F -iso-butyl  V52 (a andb) —F -sec-butyl  V53 (a and b) —F -iso-propyl  V54 (a and b) —F-n-propyl  V55 (a and b) —F -cyclohexyl  V56 (a and b) —F -tert-butoxy V57 (a and b) —F -isopropoxy  V58 (a and b) —F —CF₃  V59 (a and b) —F—CH₂CF₃  V60 (a and b) —F —OCF₃  V61 (a and b) —F —Cl  V62 (a and b) —F—Br  V63 (a and b) —F —I  V64 (a and b) —F -n-butyl  V65 (a and b) —F—CH₃  V66 (a and b) —F —SCF₃  V67 (a and b) —F —N(CH₂CH₃)₂  V68 (a andb) —F —OCF₂CHF₂  V69 (a and b) —F —C(OH)(CF₃)₂  V70 (a and b) —F-(1,1-dimethyl-pentyl)  V71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester  V72 (a and b) —F —N-piperidinyl  V73 (a and b) —CH₃ —H  V74(a and b) —CH₃ -iso-butyl  V75 (a and b) —CH₃ -tert-butyl  V76 (a and b)—CH₃ -sec-butyl  V77 (a and b) —CH₃ -iso-propyl  V78 (a and b) —CH₃-n-propyl  V79 (a and b) —CH₃ -cyclohexyl  V80 (a and b) —CH₃-tert-butoxy  V81 (a and b) —CH₃ -isopropoxy  V82 (a and b) —CH₃ —CF₃ V83 (a and b) —CH₃ —CH₂CF₃  V84 (a and b) —CH₃ —OCF₃  V85 (a and b)—CH₃ —Cl  V86 (a and b) —CH₃ —Br  V87 (a and b) —CH₃ —I  V88 (a and b)—CH₃ -n-butyl  V89 (a and b) —CH₃ —CH₃  V90 (a and b) —CH₃ —SCF₃  V91 (aand b) —CH₃ —N(CH₂CH₃)₂  V92 (a and b) —CH₃ —OCF₂CHF₂  V93 (a and b)—CH₃ —C(OH)(CF₃)₂  V94 (a and b) —CH₃ -(1,1-dimethyl-pentyl)  V95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester  V96 (a and b) —CH₃—N-piperidinyl  V97 (a and b) —CF₃ —H  V98 (a and b) —CF₃ -tert-butyl V99 (a and b) —CF₃ -iso-butyl V100 (a and b) —CF₃ -sec-butyl V101 (aand b) —CF₃ -iso-propyl V102 (a and b) —CF₃ -n-propyl V103 (a and b)—CF₃ -cyclohexyl V104 (a and b) —CF₃ -tert-butoxy V105 (a and b) —CF₃-isopropoxy V106 (a and b) —CF₃ —CF₃ V107 (a and b) —CF₃ —CH₂CF₃ V108 (aand b) —CF₃ —OCF₃ V109 (a and b) —CF₃ —Cl V110 (a and b) —CF₃ —Br V111(a and b) —CF₃ —I V112 (a and b) —CF₃ -n-butyl V113 (a and b) —CF₃ —CH₃V114 (a and b) —CF₃ —SCF₃ V115 (a and b) —CF₃ —N(CH₂CH₃)₂ V116 (a and b)—CF₃ —OCF₂CHF₂ V117 (a and b) —CF₃ —C(OH)(CF₃)₂ V118 (a and b) —CF₃-(1,1-dimethyl-pentyl) V119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester V120 (a and b) —CF₃ —N-piperidinyl V121 (a and b) —CHF₂-tert-butyl V122 (a and b) —CHF₂ —H V123 (a and b) —CHF₂ -iso-butyl V124(a and b) —CHF₂ -sec-butyl V125 (a and b) —CHF₂ -iso-propyl V126 (a andb) —CHF₂ -n-propyl V127 (a and b) —CHF₂ -cyclohexyl V128 (a and b) —CHF₂-tert-butoxy V129 (a and b) —CHF₂ -isopropoxy V130 (a and b) —CHF₂ —CF₃V131 (a and b) —CHF₂ —CH₂CF₃ V132 (a and b) —CHF₂ —OCF₃ V133 (a and b)—CHF₂ —Cl V134 (a and b) —CHF₂ —Br V135 (a and b) —CHF₂ —I V136 (a andb) —CHF₂ -n-butyl V137 (a and b) —CHF₂ —CH₃ V138 (a and b) —CHF₂ —SCF₃V139 (a and b) —CHF₂ —N(CH₂CH₃)₂ V140 (a and b) —CHF₂ —OCF₂CHF₂ V141 (aand b) —CHF₂ —C(OH)(CF₃)₂ V142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)V143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester V144 (a andb) —CHF₂ —N-piperidinyl V145 (a and b) —OH —H V146 (a and b) —OH-tert-butyl V147 (a and b) —OH -iso-butyl V148 (a and b) —OH -sec-butylV149 (a and b) —OH -iso-propyl V150 (a and b) —OH -n-propyl V151 (a andb) —OH -cyclohexyl V152 (a and b) —OH -tert-butoxy V153 (a and b) —OH-isopropoxy V154 (a and b) —OH —CF₃ V155 (a and b) —OH —CH₂CF₃ V156 (aand b) —OH —OCF₃ V157 (a and b) —OH —Cl V158 (a and b) —OH —Br V159 (aand b) —OH —I V160 (a and b) —OH -n-butyl V161 (a and b) —OH —CH₃ V162(a and b) —OH —SCF₃ V163 (a and b) —OH —N(CH₂CH₃)₂ V164 (a and b) —OH—OCF₂CHF₂ V165 (a and b) —OH —C(OH)(CF₃)₂ V166 (a and b) —OH-(1,1-dimethyl-pentyl) V167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester V168 (a and b) —OH —N-piperidinyl V169 (a and b) —NO₂ —HV170 (a and b) —NO₂ -tert-butyl V171 (a and b) —NO₂ -iso-butyl V172 (aand b) —NO₂ -sec-butyl V173 (a and b) —NO₂ -iso-propyl V174 (a and b)—NO₂ -n-propyl V175 (a and b) —NO₂ -cyclohexyl V176 (a and b) —NO₂-tert-butoxy V177 (a and b) —NO₂ -isopropoxy V178 (a and b) —NO₂ —CF₃V179 (a and b) —NO₂ —CH₂CF₃ V180 (a and b) —NO₂ —OCF₃ V181 (a and b)—NO₂ —Cl V182 (a and b) —NO₂ —Br V183 (a and b) —NO₂ —I V184 (a and b)—NO₂ -n-butyl V185 (a and b) —NO₂ —CH₃ V186 (a and b) —NO₂ —SCF₃ V187 (aand b) —NO₂ —N(CH₂CH₃)₂ V188 (a and b) —NO₂ —OCF₂CHF₂ V189 (a and b)—NO₂ —C(OH)(CF₃)₂ V190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) V191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester V192 (a and b) —NO₂—N-piperidinyl V193 (a and b) —CN —H V194 (a and b) —CN -tert-butyl V195(a and b) —CN -iso-butyl V196 (a and b) —CN -sec-butyl V197 (a and b)—CN -iso-propyl V198 (a and b) —CN -n-propyl V199 (a and b) —CN-cyclohexyl V200 (a and b) —CN -tert-butoxy V201 (a and b) —CN-isopropoxy V202 (a and b) —CN —CF₃ V203 (a and b) —CN —CH₂CF₃ V204 (aand b) —CN —OCF₃ V205 (a and b) —CN —Cl V206 (a and b) —CN —Br V207 (aand b) —CN —I V208 (a and b) —CN -n-butyl V209 (a and b) —CN —CH₃ V210(a and b) —CN —SCF₃ V211 (a and b) —CN —N(CH₂CH₃)₂ V212 (a and b) —CN—OCF₂CHF₂ V213 (a and b) —CN —C(OH)(CF₃)₂ V214 (a and b) —CN-(1,1-dimethyl-pentyl) V215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester V216 (a and b) —CN —N-piperidinyl V217 (a and b) —Br —H V218(a and b) —Br -tert-butyl V219 (a and b) —Br -iso-butyl V220 (a and b)—Br -sec-butyl V221 (a and b) —Br -iso-propyl V222 (a and b) —Br-n-propyl V223 (a and b) —Br -cyclohexyl V224 (a and b) —Br -tert-butoxyV225 (a and b) —Br -isopropoxy V226 (a and b) —Br —CF₃ V227 (a and b)—Br —CH₂CF₃ V228 (a and b) —Br —OCF₃ V229 (a and b) —Br —Cl V230 (a andb) —Br —Br V231 (a and b) —Br —I V232 (a and b) —Br -n-butyl V233 (a andb) —Br —CH₃ V234 (a and b) —Br —SCF₃ V235 (a and b) —Br —N(CH₂CH₃)₂ V236(a and b) —Br —OCF₂CHF₂ V237 (a and b) —Br —C(OH)(CF₃)₂ V238 (a and b)—Br -(1,1-dimethyl-pentyl) V239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester V240 (a and b) —Br —N-piperidinyl V241 (a and b) —I-tert-butyl V242 (a and b) —I —H V243 (a and b) —I -iso-butyl V244 (aand b) —I -sec-butyl V245 (a and b) —I -iso-propyl V246 (a and b) —I-n-propyl V247 (a and b) —I -cyclohexyl V248 (a and b) —I -tert-butoxyV249 (a and b) —I -isopropoxy V250 (a and b) —I —CF₃ V251 (a and b) —I—CH₂CF₃ V252 (a and b) —I —OCF₃ V253 (a and b) —I —Cl V254 (a and b) —I—Br V255 (a and b) —I —I V256 (a and b) —I -n-butyl V257 (a and b) —I—CH₃ V258 (a and b) —I —SCF₃ V259 (a and b) —I —N(CH₂CH₃)₂ V260 (a andb) —I —OCF₂CHF₂ V261 (a and b) —I —C(OH)(CF₃)₂ V262 (a and b) —I-(1,1-dimethyl-pentyl) V263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester V264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 23 (Iw)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b)  W1 (a and b) S —H —Cl —H  W2 (a and b) S —H —Br —H W3 (a and b) S —H —F —H  W4 (a and b) S —H —CH₃ —H  W5 (a and b) S —H—CF₃ —H  W6 (a and b) S —H —OCH₃ —H  W7 (a and b) S —H —OCH₂CH₃ —H  W8(a and b) S —H —OCF₃ —H  W9 (a and b) S —H -tert-butyl —H  W10 (a and b)S —H -iso-propyl —H  W11 (a and b) S —H —CH₃ —CH₃  W12 (a and b) S —H —H—H  W13 (a and b) S —H —H —Cl  W14 (a and b) S —H —H —Br  W15 (a and b)S —H —H —F  W16 (a and b) S —H —H —CH₃  W17 (a and b) S —H —H —CF₃  W18(a and b) S —H —H —OCH₃  W19 (a and b) S —H —H —OCH₂CH₃  W20 (a and b) S—H —H —OCF₃  W21 (a and b) S —H —H -tert-butyl  W22 (a and b) S —H —H-iso-propyl  W23 (a and b) S —Cl —Cl —H  W24 (a and b) S —Cl —Br —H  W25(a and b) S —Cl —F —H  W26 (a and b) S —Cl —CH₃ —H  W27 (a and b) S —Cl—CF₃ —H  W28 (a and b) S —Cl —OCH₃ —H  W29 (a and b) S —Cl —OCH₂CH₃ —H W30 (a and b) S —Cl —OCF₃ —H  W31 (a and b) S —Cl -tert-butyl —H  W32(a and b) S —Cl -iso-propyl —H  W33 (a and b) S —Cl —CH₃ —CH₃  W34 (aand b) S —Cl —H —H  W35 (a and b) S —Cl —H —Cl  W36 (a and b) S —Cl —H—Br  W37 (a and b) S —Cl —H —F  W38 (a and b) S —Cl —H —CH₃  W39 (a andb) S —Cl —H —CF₃  W40 (a and b) S —Cl —H —OCH₃  W41 (a and b) S —Cl —H—OCH₂CH₃  W42 (a and b) S —Cl —H —OCF₃  W43 (a and b) S —Cl —H-tert-butyl  W44 (a and b) S —Cl —H -iso-propyl  W45 (a and b) S —Cl —H—OCF₃  W46 (a and b) S —Cl —H -tert-butyl  W47 (a and b) S —Cl —H-iso-propyl  W48 (a and b) S —CH₃ —Cl —H  W49 (a and b) S —CH₃ —Br —H W50 (a and b) S —CH₃ —F —H  W51 (a and b) S —CH₃ —CH₃ —H  W52 (a and b)S —CH₃ —CF₃ —H  W53 (a and b) S —CH₃ —OCH₃ —H  W54 (a and b) S —CH₃—OCH₂CH₃ —H  W55 (a and b) S —CH₃ —OCF₃ —H  W56 (a and b) S —CH₃-tert-butyl —H  W57 (a and b) S —CH₃ -iso-propyl —H  W58 (a and b) S—CH₃ —CH₃ —CH₃  W59 (a and b) S —CH₃ —H —H  W60 (a and b) S —CH₃ —H —Cl W61 (a and b) S —CH₃ —H —Br  W62 (a and b) S —CH₃ —H —F  W63 (a and b)S —CH₃ —H —CH₃  W64 (a and b) S —CH₃ —H —CF₃  W65 (a and b) S —CH₃ —H—OCH₃  W66 (a and b) S —CH₃ —H —OCH₂CH₃  W67 (a and b) S —CH₃ —H —OCF₃ W68 (a and b) S —CH₃ —H -tert-butyl  W69 (a and b) S —CH₃ —H-iso-propyl  W70 (a and b) S —CF₃ —Cl —H  W71 (a and b) S —CF₃ —Br —H W72 (a and b) S —CF₃ —F —H  W73 (a and b) S —CF₃ —CH₃ —H  W74 (a and b)S —CF₃ —CF₃ —H  W75 (a and b) S —CF₃ —OCH₃ —H  W76 (a and b) S —CF₃—OCH₂CH₃ —H  W77 (a and b) S —CF₃ —OCF₃ —H  W78 (a and b) S —CF₃-tert-butyl —H  W79 (a and b) S —CF₃ -iso-propyl —H  W80 (a and b) S—CF₃ —CH₃ —CH₃  W81 (a and b) S —CF₃ —H —H  W82 (a and b) S —CF₃ —H —Cl W83 (a and b) S —CF₃ —H —Br  W84 (a and b) S —CF₃ —H —F  W85 (a and b)S —CF₃ —H —CH₃  W86 (a and b) S —CF₃ —H —CF₃  W87 (a and b) S —CF₃ —H—OCH₃  W88 (a and b) S —CF₃ —H —OCH₂CH₃  W89 (a and b) S —CF₃ —H —OCF₃ W90 (a and b) S —CF₃ —H -tert-butyl  W91 (a and b) S —CF₃ —H-iso-propyl  W92 (a and b) S —CHF₂ —Cl —H  W93 (a and b) S —CHF₂ —Br —H W94 (a and b) S —CHF₂ —F —H  W95 (a and b) S —CHF₂ —CH₃ —H  W96 (a andb) S —CHF₂ —CF₃ —H  W97 (a and b) S —CHF₂ —OCH₃ —H  W98 (a and b) S—CHF₂ —OCH₂CH₃ —H  W99 (a and b) S —CHF₂ —OCF₃ —H W100 (a and b) S —CHF₂-tert-butyl —H W101 (a and b) S —CHF₂ -iso-propyl —H W102 (a and b) S—CHF₂ —CH₃ —CH₃ W103 (a and b) S —CHF₂ —H —H W104 (a and b) S —CHF₂ —H—Cl W105 (a and b) S —CHF₂ —H —Br W106 (a and b) S —CHF₂ —H —F W107 (aand b) S —CHF₂ —H —CH₃ W108 (a and b) S —CHF₂ —H —CF₃ W109 (a and b) S—CHF₂ —H —OCH₃ W110 (a and b) S —CHF₂ —H —OCH₂CH₃ W111 (a and b) S —CHF₂—H —OCF₃ W112 (a and b) S —CHF₂ —H -tert-butyl W113 (a and b) S —CHF₂ —H-iso-propyl W114 (a and b) S —OH —Cl —H W115 (a and b) S —OH —Br —H W116(a and b) S —OH —F —H W117 (a and b) S —OH —CH₃ —H W118 (a and b) S —OH—CF₃ —H W119 (a and b) S —OH —OCH₃ —H W120 (a and b) S —OH —OCH₂CH₃ —HW121 (a and b) S —OH —OCF₃ —H W122 (a and b) S —OH -tert-butyl —H W123(a and b) S —OH -iso-propyl —H W124 (a and b) S —OH —CH₃ —CH₃ W125 (aand b) S —OH —H —H W126 (a and b) S —OH —H —Cl W127 (a and b) S —OH —H—Br W128 (a and b) S —OH —H —F W129 (a and b) S —OH —H —CH₃ W130 (a andb) S —OH —H —CF₃ W131 (a and b) S —OH —H —OCH₃ W132 (a and b) S —OH —H—OCH₂CH₃ W133 (a and b) S —OH —H —OCF₃ W134 (a and b) S —OH —H-tert-butyl W135 (a and b) S —OH —H -iso-propyl W136 (a and b) S —NO₂—Cl —H W137 (a and b) S —NO₂ —Br —H W138 (a and b) S —NO₂ —F —H W139 (aand b) S —NO₂ —CH₃ —H W140 (a and b) S —NO₂ —CF₃ —H W141 (a and b) S—NO₂ —OCH₃ —H W142 (a and b) S —NO₂ —OCH₂CH₃ —H W143 (a and b) S —NO₂—OCF₃ —H W144 (a and b) S —NO₂ -tert-butyl —H W145 (a and b) S —NO₂-iso-propyl —H W146 (a and b) S —NO₂ —CH₃ —CH₃ W147 (a and b) S —NO₂ —H—H W148 (a and b) S —NO₂ —H —Cl W149 (a and b) S —NO₂ —H —Br W150 (a andb) S —NO₂ —H —F W151 (a and b) S —NO₂ —H —CH₃ W152 (a and b) S —NO₂ —H—CF₃ W153 (a and b) S —NO₂ —H —OCH₃ W154 (a and b) S —NO₂ —H —OCH₂CH₃W155 (a and b) S —NO₂ —H —OCF₃ W156 (a and b) S —NO₂ —H -tert-butyl W157(a and b) S —NO₂ —H -iso-propyl W158 (a and b) S —CN —Br —H W159 (a andb) S —CN —Cl —H W160 (a and b) S —CN —F —H W161 (a and b) S —CN —CH₃ —HW162 (a and b) S —CN —CF₃ —H W163 (a and b) S —CN —OCH₃ —H W164 (a andb) S —CN —OCH₂CH₃ —H W165 (a and b) S —CN —OCF₃ —H W166 (a and b) S —CN-tert-butyl —H W167 (a and b) S —CN -iso-propyl —H W168 (a and b) S —CN—CH₃ —CH₃ W169 (a and b) S —CN —H —H W170 (a and b) S —CN —H —Cl W171 (aand b) S —CN —H —Br W172 (a and b) S —CN —H —F W173 (a and b) S —CN —H—CH₃ W174 (a and b) S —CN —H —CF₃ W175 (a and b) S —CN —H —OCH₃ W176 (aand b) S —CN —H —OCH₂CH₃ W177 (a and b) S —CN —H —OCF₃ W178 (a and b) S—CN —H -tert-butyl W179 (a and b) S —CN —H -iso-propyl W180 (a and b) S—Br —Br —H W181 (a and b) S —Br —Cl —H W182 (a and b) S —Br —F —H W183(a and b) S —Br —CH₃ —H W184 (a and b) S —Br —CF₃ —H W185 (a and b) S—Br —OCH₃ —H W186 (a and b) S —Br —OCH₂CH₃ —H W187 (a and b) S —Br —OCF₃—H W188 (a and b) S —Br -tert-butyl —H W189 (a and b) S —Br -iso-propyl—H W190 (a and b) S —Br —CH₃ —CH₃ W191 (a and b) S —Br —H —H W192 (a andb) S —Br —H —Cl W193 (a and b) S —Br —H —Br W194 (a and b) S —Br —H —FW195 (a and b) S —Br —H —CH₃ W196 (a and b) S —Br —H —CF₃ W197 (a and b)S —Br —H —OCH₃ W198 (a and b) S —Br —H —OCH₂CH₃ W199 (a and b) S —Br —H—OCF₃ W200 (a and b) S —Br —H -tert-butyl W201 (a and b) S —Br —H-iso-propyl W202 (a and b) S —I —Cl —H W203 (a and b) S —I —Br —H W204(a and b) S —I —F —H W205 (a and b) S —I —CH₃ —H W206 (a and b) S —I—CF₃ —H W207 (a and b) S —I —OCH₃ —H W208 (a and b) S —I —OCH₂CH₃ —HW209 (a and b) S —I —OCF₃ —H W210 (a and b) S —I -tert-butyl —H W211 (aand b) S —I -iso-propyl —H W212 (a and b) S —I —CH₃ —CH₃ W213 (a and b)S —I —H —H W214 (a and b) S —I —H —Cl W215 (a and b) S —I —H —Br W216 (aand b) S —I —H —F W217 (a and b) S —I —H —CH₃ W218 (a and b) S —I —H—CF₃ W219 (a and b) S —I —H —OCH₃ W220 (a and b) S —I —H —OCH₂CH₃ W221(a and b) S —I —H —OCF₃ W222 (a and b) S —I —H -tert-butyl W223 (a andb) S —I —H -iso-propyl W224 (a and b) O —H —Cl —H W225 (a and b) O —H—Br —H W226 (a and b) O —H —F —H W227 (a and b) O —H —CH₃ —H W228 (a andb) O —H —CF₃ —H W229 (a and b) O —H —OCH₃ —H W230 (a and b) O —H—OCH₂CH₃ —H W231 (a and b) O —H —OCF₃ —H W232 (a and b) O —H -tert-butyl—H W233 (a and b) O —H -iso-propyl —H W234 (a and b) O —H —CH₃ —CH₃ W235(a and b) O —H —H —H W236 (a and b) O —H —H —Cl W237 (a and b) O —H —H—Br W238 (a and b) O —H —H —F W239 (a and b) O —H —H —CH₃ W240 (a and b)O —H —H —CF₃ W241 (a and b) O —H —H —OCH₃ W242 (a and b) O —H —H—OCH₂CH₃ W243 (a and b) O —H —H —OCF₃ W244 (a and b) O —H —H -tert-butylW245 (a and b) O —H —H -iso-propyl W246 (a and b) O —Cl —Cl —H W247 (aand b) O —Cl —Br —H W248 (a and b) O —Cl —F —H W249 (a and b) O —Cl —CH₃—H W250 (a and b) O —Cl —CF₃ —H W251 (a and b) O —Cl —OCH₃ —H W252 (aand b) O —Cl —OCH₂CH₃ —H W253 (a and b) O —Cl —OCF₃ —H W254 (a and b) O—Cl -tert-butyl —H W255 (a and b) O —Cl -iso-propyl —H W256 (a and b) O—Cl —CH₃ —CH₃ W257 (a and b) O —Cl —H —H W258 (a and b) O —Cl —H —CH₃W259 (a and b) O —Cl —H —Cl W260 (a and b) O —Cl —H —Br W261 (a and b) O—Cl —H —F W262 (a and b) O —Cl —H —CF₃ W263 (a and b) O —Cl —H —OCH₃W264 (a and b) O —Cl —H —OCH₂CH₃ W265 (a and b) O —Cl —H —OCF₃ W266 (aand b) O —Cl —H -tert-butyl W267 (a and b) O —Cl —H -iso-propyl W268 (aand b) O —Cl —H —OCF₃ W269 (a and b) O —Cl —H -tert-butyl W270 (a and b)O —Cl —H -iso-propyl W271 (a and b) O —CH₃ —Cl —H W272 (a and b) O —CH₃—Br —H W273 (a and b) O —CH₃ —F —H W274 (a and b) O —CH₃ —CH₃ —H W275 (aand b) O —CH₃ —CF₃ —H W276 (a and b) O —CH₃ —OCH₃ —H W277 (a and b) O—CH₃ —OCH₂CH₃ —H W278 (a and b) O —CH₃ —OCF₃ —H W279 (a and b) O —CH₃-tert-butyl —H W280 (a and b) O —CH₃ -iso-propyl —H W281 (a and b) O—CH₃ —CH₃ —CH₃ W282 (a and b) O —CH₃ —H —H W283 (a and b) O —CH₃ —H —ClW284 (a and b) O —CH₃ —H —Br W285 (a and b) O —CH₃ —H —F W286 (a and b)O —CH₃ —H —CH₃ W287 (a and b) O —CH₃ —H —CF₃ W288 (a and b) O —CH₃ —H—OCH₃ W289 (a and b) O —CH₃ —H —OCH₂CH₃ W290 (a and b) O —CH₃ —H —OCF₃W291 (a and b) O —CH₃ —H -tert-butyl W292 (a and b) O —CH₃ —H-iso-propyl W293 (a and b) O —CF₃ —Cl —H W294 (a and b) O —CF₃ —Br —HW295 (a and b) O —CF₃ —F —H W296 (a and b) O —CF₃ —CH₃ —H W297 (a and b)O —CF₃ —CF₃ —H W298 (a and b) O —CF₃ —OCH₃ —H W299 (a and b) O —CF₃—OCH₂CH₃ —H W300 (a and b) O —CF₃ —OCF₃ —H W301 (a and b) O —CF₃-tert-butyl —H W302 (a and b) O —CF₃ -iso-propyl —H W303 (a and b) O—CF₃ —CH₃ —CH₃ W304 (a and b) O —CF₃ —H —H W305 (a and b) O —CF₃ —H —ClW306 (a and b) O —CF₃ —H —Br W307 (a and b) O —CF₃ —H —F W308 (a and b)O —CF₃ —H —CH₃ W309 (a and b) O —CF₃ —H —CF₃ W310 (a and b) O —CF₃ —H—OCH₃ W311 (a and b) O —CF₃ —H —OCH₂CH₃ W312 (a and b) O —CF₃ —H —OCF₃W313 (a and b) O —CF₃ —H -tert-butyl W314 (a and b) O —CF₃ —H-iso-propyl W315 (a and b) O —CHF₂ —Cl —H W316 (a and b) O —CHF₂ —Br —HW317 (a and b) O —CHF₂ —F —H W318 (a and b) O —CHF₂ —CH₃ —H W319 (a andb) O —CHF₂ —CF₃ —H W320 (a and b) O —CHF₂ —OCH₃ —H W321 (a and b) O—CHF₂ —OCH₂CH₃ —H W322 (a and b) O —CHF₂ —OCF₃ —H W323 (a and b) O —CHF₂-tert-butyl —H W324 (a and b) O —CHF₂ -iso-propyl —H W325 (a and b) O—CHF₂ —CH₃ —CH₃ W326 (a and b) O —CHF₂ —H —H W327 (a and b) O —CHF₂ —H—Cl W328 (a and b) O —CHF₂ —H —Br W329 (a and b) O —CHF₂ —H —F W330 (aand b) O —CHF₂ —H —CH₃ W331 (a and b) O —CHF₂ —H —CF₃ W332 (a and b) O—CHF₂ —H —OCH₃ W333 (a and b) O —CHF₂ —H —OCH₂CH₃ W334 (a and b) O —CHF₂—H —OCF₃ W335 (a and b) O —CHF₂ —H -tert-butyl W336 (a and b) O —CHF₂ —H-iso-propyl W337 (a and b) O —OH —Cl —H W338 (a and b) O —OH —Br —H W339(a and b) O —OH —F —H W340 (a and b) O —OH —CH₃ —H W341 (a and b) O —OH—CF₃ —H W342 (a and b) O —OH —OCH₃ —H W343 (a and b) O —OH —OCH₂CH₃ —HW344 (a and b) O —OH —OCF₃ —H W345 (a and b) O —OH -tert-butyl —H W346(a and b) O —OH -iso-propyl —H W347 (a and b) O —OH —CH₃ —CH₃ W348 (aand b) O —OH —H —H W349 (a and b) O —OH —H —Cl W350 (a and b) O —OH —H—Br W351 (a and b) O —OH —H —F W352 (a and b) O —OH —H —CH₃ W353 (a andb) O —OH —H —CF₃ W354 (a and b) O —OH —H —OCH₃ W355 (a and b) O —OH —H—OCH₂CH₃ W356 (a and b) O —OH —H —OCF₃ W357 (a and b) O —OH —H-tert-butyl W358 (a and b) O —OH —H -iso-propyl W359 (a and b) O —NO₂—Cl —H W360 (a and b) O —NO₂ —Br —H W361 (a and b) O —NO₂ —F —H W362 (aand b) O —NO₂ —CH₃ —H W363 (a and b) O —NO₂ —CF₃ —H W364 (a and b) O—NO₂ —OCH₃ —H W365 (a and b) O —NO₂ —OCH₂CH₃ —H W366 (a and b) O —NO₂—OCF₃ —H W367 (a and b) O —NO₂ -tert-butyl —H W368 (a and b) O —NO₂-iso-propyl —H W369 (a and b) O —NO₂ —CH₃ —CH₃ W370 (a and b) O —NO₂ —H—H W371 (a and b) O —NO₂ —H —Cl W372 (a and b) O —NO₂ —H —Br W373 (a andb) O —NO₂ —H —F W374 (a and b) O —NO₂ —H —CH₃ W375 (a and b) O —NO₂ —H—CF₃ W376 (a and b) O —NO₂ —H —OCH₃ W377 (a and b) O —NO₂ —H —OCH₂CH₃W378 (a and b) O —NO₂ —H —OCF₃ W379 (a and b) O —NO₂ —H -tert-butyl W380(a and b) O —NO₂ —H -iso-propyl W381 (a and b) O —CN —Br —H W382 (a andb) O —CN —Cl —H W383 (a and b) O —CN —F —H W384 (a and b) O —CN —CH₃ —HW385 (a and b) O —CN —CF₃ —H W386 (a and b) O —CN —OCH₃ —H W387 (a andb) O —CN —OCH₂CH₃ —H W388 (a and b) O —CN —OCF₃ —H W389 (a and b) O —CN-tert-butyl —H W390 (a and b) O —CN -iso-propyl —H W391 (a and b) O —CN—CH₃ —CH₃ W392 (a and b) O —CN —H —H W393 (a and b) O —CN —H —Cl W394 (aand b) O —CN —H —Br W395 (a and b) O —CN —H —F W396 (a and b) O —CN —H—CH₃ W397 (a and b) O —CN —H —CF₃ W398 (a and b) O —CN —H —OCH₃ W399 (aand b) O —CN —H —OCH₂CH₃ W400 (a and b) O —CN —H —OCF₃ W401 (a and b) O—CN —H -tert-butyl W402 (a and b) O —CN —H -iso-propyl W403 (a and b) O—Br —Br —H W404 (a and b) O —Br —Cl —H W405 (a and b) O —Br —F —H W406(a and b) O —Br —CH₃ —H W407 (a and b) O —Br —CF₃ —H W408 (a and b) O—Br —OCH₃ —H W409 (a and b) O —Br —OCH₂CH₃ —H W410 (a and b) O —Br —OCF₃—H W411 (a and b) O —Br -tert-butyl —H W412 (a and b) O —Br -iso-propyl—H W413 (a and b) O —Br —CH₃ —CH₃ W414 (a and b) O —Br —H —H W415 (a andb) O —Br —H —Cl W416 (a and b) O —Br —H —Br W417 (a and b) O —Br —H —FW418 (a and b) O —Br —H —CH₃ W419 (a and b) O —Br —H —CF₃ W420 (a and b)O —Br —H —OCH₃ W421 (a and b) O —Br —H —OCH₂CH₃ W422 (a and b) O —Br —H—OCF₃ W423 (a and b) O —Br —H -tert-butyl W424 (a and b) O —Br —H-iso-propyl W425 (a and b) O —I —Cl —H W426 (a and b) O —I —Br —H W427(a and b) O —I —F —H W428 (a and b) O —I —CH₃ —H W429 (a and b) O —I—CF₃ —H W430 (a and b) O —I —OCH₃ —H W431 (a and b) O —I —OCH₂CH₃ —HW432 (a and b) O —I —OCF₃ —H W433 (a and b) O —I -tert-butyl —H W434 (aand b) O —I -iso-propyl —H W435 (a and b) O —I —CH₃ —CH₃ W436 (a and b)O —I —H —H W437 (a and b) O —I —H —Cl W438 (a and b) O —I —H —Br W439 (aand b) O —I —H —F W440 (a and b) O —I —H —CH₃ W441 (a and b) O —I —H—CF₃ W442 (a and b) O —I —H —OCH₃ W443 (a and b) O —I —H —OCH₂CH₃ W444(a and b) O —I —H —OCF₃ W445 (a and b) O —I —H -tert-butyl W446 (a andb) O —I —H -iso-propyl W447 (a and b) NH —H —Cl —H W448 (a and b) NH —H—Br —H W449 (a and b) NH —H —F —H W450 (a and b) NH —H —CH₃ —H W451 (aand b) NH —H —CF₃ —H W452 (a and b) NH —H —OCH₃ —H W453 (a and b) NH —H—OCH₂CH₃ —H W454 (a and b) NH —H —OCF₃ —H W455 (a and b) NH —H-tert-butyl —H W456 (a and b) NH —H -iso-propyl —H W457 (a and b) NH —H—CH₃ —CH₃ W458 (a and b) NH —H —H —H W459 (a and b) NH —H —H —Cl W460 (aand b) NH —H —H —Br W461 (a and b) NH —H —H —F W462 (a and b) NH —H —H—CH₃ W463 (a and b) NH —H —H —CF₃ W464 (a and b) NH —H —H —OCH₃ W465 (aand b) NH —H —H —OCH₂CH₃ W466 (a and b) NH —H —H —OCF₃ W467 (a and b) NH—H —H -tert-butyl W468 (a and b) NH —H —H -iso-propyl W469 (a and b) NH—Cl —Cl —H W470 (a and b) NH —Cl —Br —H W471 (a and b) NH —Cl —F —H W472(a and b) NH —Cl —CH₃ —H W473 (a and b) NH —Cl —CF₃ —H W474 (a and b) NH—Cl —OCH₃ —H W475 (a and b) NH —Cl —OCH₂CH₃ —H W476 (a and b) NH —Cl—OCF₃ —H W477 (a and b) NH —Cl -tert-butyl —H W478 (a and b) NH —Cl-iso-propyl —H W479 (a and b) NH —Cl —CH₃ —CH₃ W480 (a and b) NH —Cl —H—H W481 (a and b) NH —Cl —H —CH₃ W482 (a and b) NH —Cl —H —Cl W483 (aand b) NH —Cl —H —Br W484 (a and b) NH —Cl —H —F W485 (a and b) NH —Cl—H —CF₃ W486 (a and b) NH —Cl —H —OCH₃ W487 (a and b) NH —Cl —H —OCH₂CH₃W488 (a and b) NH —Cl —H —OCF₃ W489 (a and b) NH —Cl —H -tert-butyl W490(a and b) NH —Cl —H -iso-propyl W491 (a and b) NH —Cl —H —OCF₃ W492 (aand b) NH —Cl —H -tert-butyl W493 (a and b) NH —Cl —H -iso-propyl W494(a and b) NH —CH₃ —Cl —H W495 (a and b) NH —CH₃ —Br —H W496 (a and b) NH—CH₃ —F —H W497 (a and b) NH —CH₃ —CH₃ —H W498 (a and b) NH —CH₃ —CF₃ —HW499 (a and b) NH —CH₃ —OCH₃ —H W500 (a and b) NH —CH₃ —OCH₂CH₃ —H W501(a and b) NH —CH₃ —OCF₃ —H W502 (a and b) NH —CH₃ -tert-butyl —H W503 (aand b) NH —CH₃ -iso-propyl —H W504 (a and b) NH —CH₃ —CH₃ —CH₃ W505 (aand b) NH —CH₃ —H —H W506 (a and b) NH —CH₃ —H —Cl W507 (a and b) NH—CH₃ —H —Br W508 (a and b) NH —CH₃ —H —F W509 (a and b) NH —CH₃ —H —CH₃W510 (a and b) NH —CH₃ —H —CF₃ W511 (a and b) NH —CH₃ —H —OCH₃ W512 (aand b) NH —CH₃ —H —OCH₂CH₃ W513 (a and b) NH —CH₃ —H —OCF₃ W514 (a andb) NH —CH₃ —H -tert-butyl W515 (a and b) NH —CH₃ —H -iso-propyl W516 (aand b) NH —CF₃ —Cl —H W517 (a and b) NH —CF₃ —Br —H W518 (a and b) NH—CF₃ —F —H W519 (a and b) NH —CF₃ —CH₃ —H W520 (a and b) NH —CF₃ —CF₃ —HW521 (a and b) NH —CF₃ —OCH₃ —H W522 (a and b) NH —CF₃ —OCH₂CH₃ —H W523(a and b) NH —CF₃ —OCF₃ —H W524 (a and b) NH —CF₃ -tert-butyl —H W525 (aand b) NH —CF₃ -iso-propyl —H W526 (a and b) NH —CF₃ —CH₃ —CH₃ W527 (aand b) NH —CF₃ —H —H W528 (a and b) NH —CF₃ —H —Cl W529 (a and b) NH—CF₃ —H —Br W530 (a and b) NH —CF₃ —H —F W531 (a and b) NH —CF₃ —H —CH₃W532 (a and b) NH —CF₃ —H —CF₃ W533 (a and b) NH —CF₃ —H —OCH₃ W534 (aand b) NH —CF₃ —H —OCH₂CH₃ W535 (a and b) NH —CF₃ —H —OCF₃ W536 (a andb) NH —CF₃ —H -tert-butyl W537 (a and b) NH —CF₃ —H -iso-propyl W538 (aand b) NH —CHF₂ —Cl —H W539 (a and b) NH —CHF₂ —Br —H W540 (a and b) NH—CHF₂ —F —H W541 (a and b) NH —CHF₂ —CH₃ —H W542 (a and b) NH —CHF₂ —CF₃—H W543 (a and b) NH —CHF₂ —OCH₃ —H W544 (a and b) NH —CHF₂ —OCH₂CH₃ —HW545 (a and b) NH —CHF₂ —OCF₃ —H W546 (a and b) NH —CHF₂ -tert-butyl —HW547 (a and b) NH —CHF₂ -iso-propyl —H W548 (a and b) NH —CHF₂ —CH₃ —CH₃W549 (a and b) NH —CHF₂ —H —H W550 (a and b) NH —CHF₂ —H —Cl W551 (a andb) NH —CHF₂ —H —Br W552 (a and b) NH —CHF₂ —H —F W553 (a and b) NH —CHF₂—H —CH₃ W554 (a and b) NH —CHF₂ —H —CF₃ W555 (a and b) NH —CHF₂ —H —OCH₃W556 (a and b) NH —CHF₂ —H —OCH₂CH₃ W557 (a and b) NH —CHF₂ —H —OCF₃W558 (a and b) NH —CHF₂ —H -tert-butyl W559 (a and b) NH —CHF₂ —H-iso-propyl W560 (a and b) NH —OH —Cl —H W561 (a and b) NH —OH —Br —HW562 (a and b) NH —OH —F —H W563 (a and b) NH —OH —CH₃ —H W564 (a and b)NH —OH —CF₃ —H W565 (a and b) NH —OH —OCH₃ —H W566 (a and b) NH —OH—OCH₂CH₃ —H W567 (a and b) NH —OH —OCF₃ —H W568 (a and b) NH —OH-tert-butyl —H W569 (a and b) NH —OH -iso-propyl —H W570 (a and b) NH—OH —CH₃ —CH₃ W571 (a and b) NH —OH —H —H W572 (a and b) NH —OH —H —ClW573 (a and b) NH —OH —H —Br W574 (a and b) NH —OH —H —F W575 (a and b)NH —OH —H —CH₃ W576 (a and b) NH —OH —H —CF₃ W577 (a and b) NH —OH —H—OCH₃ W578 (a and b) NH —OH —H —OCH₂CH₃ W579 (a and b) NH —OH —H —OCF₃W580 (a and b) NH —OH —H -tert-butyl W581 (a and b) NH —OH —H-iso-propyl W582 (a and b) NH —NO₂ —Cl —H W583 (a and b) NH —NO₂ —Br —HW584 (a and b) NH —NO₂ —F —H W585 (a and b) NH —NO₂ —CH₃ —H W586 (a andb) NH —NO₂ —CF₃ —H W587 (a and b) NH —NO₂ —OCH₃ —H W588 (a and b) NH—NO₂ —OCH₂CH₃ —H W589 (a and b) NH —NO₂ —OCF₃ —H W590 (a and b) NH —NO₂-tert-butyl —H W591 (a and b) NH —NO₂ -iso-propyl —H W592 (a and b) NH—NO₂ —CH₃ —CH₃ W593 (a and b) NH —NO₂ —H —H W594 (a and b) NH —NO₂ —H—Cl W595 (a and b) NH —NO₂ —H —Br W596 (a and b) NH —NO₂ —H —F W597 (aand b) NH —NO₂ —H —CH₃ W598 (a and b) NH —NO₂ —H —CF₃ W599 (a and b) NH—NO₂ —H —OCH₃ W600 (a and b) NH —NO₂ —H —OCH₂CH₃ W601 (a and b) NH —NO₂—H —OCF₃ W602 (a and b) NH —NO₂ —H -tert-butyl W603 (a and b) NH —NO₂ —H-iso-propyl W604 (a and b) NH —CN —Br —H W605 (a and b) NH —CN —Cl —HW606 (a and b) NH —CN —F —H W607 (a and b) NH —CN —CH₃ —H W608 (a and b)NH —CN —CF₃ —H W609 (a and b) NH —CN —OCH₃ —H W610 (a and b) NH —CN—OCH₂CH₃ —H W611 (a and b) NH —CN —OCF₃ —H W612 (a and b) NH —CN-tert-butyl —H W613 (a and b) NH —CN -iso-propyl —H W614 (a and b) NH—CN —CH₃ —CH₃ W615 (a and b) NH —CN —H —H W616 (a and b) NH —CN —H —ClW617 (a and b) NH —CN —H —Br W618 (a and b) NH —CN —H —F W619 (a and b)NH —CN —H —CH₃ W620 (a and b) NH —CN —H —CF₃ W621 (a and b) NH —CN —H—OCH₃ W622 (a and b) NH —CN —H —OCH₂CH₃ W623 (a and b) NH —CN —H —OCF₃W624 (a and b) NH —CN —H -tert-butyl W625 (a and b) NH —CN —H-iso-propyl W626 (a and b) NH —Br —Br —H W627 (a and b) NH —Br —Cl —HW628 (a and b) NH —Br —F —H W629 (a and b) NH —Br —CH₃ —H W630 (a and b)NH —Br —CF₃ —H W631 (a and b) NH —Br —OCH₃ —H W632 (a and b) NH —Br—OCH₂CH₃ —H W633 (a and b) NH —Br —OCF₃ —H W634 (a and b) NH —Br-tert-butyl —H W635 (a and b) NH —Br -iso-propyl —H W636 (a and b) NH—Br —CH₃ —CH₃ W637 (a and b) NH —Br —H —H W638 (a and b) NH —Br —H —ClW639 (a and b) NH —Br —H —Br W640 (a and b) NH —Br —H —F W641 (a and b)NH —Br —H —CH₃ W642 (a and b) NH —Br —H —CF₃ W643 (a and b) NH —Br —H—OCH₃ W644 (a and b) NH —Br —H —OCH₂CH₃ W645 (a and b) NH —Br —H —OCF₃W646 (a and b) NH —Br —H -tert-butyl W647 (a and b) NH —Br —H-iso-propyl W648 (a and b) NH —I —Cl —H W649 (a and b) NH —I —Br —H W650(a and b) NH —I —F —H W651 (a and b) NH —I —CH₃ —H W652 (a and b) NH —I—CF₃ —H W653 (a and b) NH —I —OCH₃ —H W654 (a and b) NH —I —OCH₂CH₃ —HW655 (a and b) NH —I —OCF₃ —H W656 (a and b) NH —I -tert-butyl —H W657(a and b) NH —I -iso-propyl —H W658 (a and b) NH —I —CH₃ —CH₃ W659 (aand b) NH —I —H —H W660 (a and b) NH —I —H —Cl W661 (a and b) NH —I —H—Br W662 (a and b) NH —I —H —F W663 (a and b) NH —I —H —CH₃ W664 (a andb) NH —I —H —CF₃ W665 (a and b) NH —I —H —OCH₃ W666 (a and b) NH —I —H—OCH₂CH₃ W667 (a and b) NH —I —H —OCF₃ W668 (a and b) NH —I —H-tert-butyl W669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 24 (Ix)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  X1 (a and b) —H —H  X2 (a and b) —H -tert-butyl  X3 (a and b) —H-iso-butyl  X4 (a and b) —H -sec-butyl  X5 (a and b) —H -iso-propyl  X6(a and b) —H -n-propyl  X7 (a and b) —H -cyclohexyl  X8 (a and b) —H-tert-butoxy  X9 (a and b) —H -isopropoxy  X10 (a and b) —H —CF₃  X11 (aand b) —H —CH₂CF₃  X12 (a and b) —H —OCF₃  X13 (a and b) —H —Cl  X14 (aand b) —H —Br  X15 (a and b) —H —I  X16 (a and b) —H -n-butyl  X17 (aand b) —H —CH₃  X18 (a and b) —H —SCF₃  X19 (a and b) —H —N(CH₂CH₃)₂ X20 (a and b) —H —OCF₂CHF₂  X21 (a and b) —H —C(OH)(CF₃)₂  X22 (a andb) —H -(1,1-dimethyl-pentyl)  X23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester  X24 (a and b) —H —N-piperidinyl  X25 (a and b) —Cl —H X26 (a and b) —Cl -tert-butyl  X27 (a and b) —Cl -iso-butyl  X28 (a andb) —Cl -sec-butyl  X29 (a and b) —Cl -iso-propyl  X30 (a and b) —Cl-n-propyl  X31 (a and b) —Cl -cyclohexyl  X32 (a and b) —Cl -tert-butoxy X33 (a and b) —Cl -isopropoxy  X34 (a and b) —Cl —CF₃  X35 (a and b)—Cl —CH₂CF₃  X36 (a and b) —Cl —OCF₃  X37 (a and b) —Cl —Cl  X38 (a andb) —Cl —Br  X39 (a and b) —Cl —I  X40 (a and b) —Cl -n-butyl  X41 (a andb) —Cl —CH₃  X42 (a and b) —Cl —SCF₃  X43 (a and b) —Cl —N(CH₂CH₃)₂  X44(a and b) —Cl —OCF₂CHF₂  X45 (a and b) —Cl —C(OH)(CF₃)₂  X46 (a and b)—Cl -(1,1-dimethyl-pentyl)  X47 (a and b) —Cl -(1,1-dimethyl-aceticacid) ethyl ester  X48 (a and b) —Cl —N-piperidinyl  X49 (a and b) —F —H X50 (a and b) —F -tert-butyl  X51 (a and b) —F -iso-butyl  X52 (a andb) —F -sec-butyl  X53 (a and b) —F -iso-propyl  X54 (a and b) —F-n-propyl  X55 (a and b) —F -cyclohexyl  X56 (a and b) —F -tert-butoxy X57 (a and b) —F -isopropoxy  X58 (a and b) —F —CF₃  X59 (a and b) —F—CH₂CF₃  X60 (a and b) —F —OCF₃  X61 (a and b) —F —Cl  X62 (a and b) —F—Br  X63 (a and b) —F —I  X64 (a and b) —F -n-butyl  X65 (a and b) —F—CH₃  X66 (a and b) —F —SCF₃  X67 (a and b) —F —N(CH₂CH₃)₂  X68 (a andb) —F —OCF₂CHF₂  X69 (a and b) —F —C(OH)(CF₃)₂  X70 (a and b) —F-(1,1-dimethyl-pentyl)  X71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester  X72 (a and b) —F —N-piperidinyl  X73 (a and b) —CH₃ —H  X74(a and b) —CH₃ -iso-butyl  X75 (a and b) —CH₃ -tert-butyl  X76 (a and b)—CH₃ -sec-butyl  X77 (a and b) —CH₃ -iso-propyl  X78 (a and b) —CH₃-n-propyl  X79 (a and b) —CH₃ -cyclohexyl  X80 (a and b) —CH₃-tert-butoxy  X81 (a and b) —CH₃ -isopropoxy  X82 (a and b) —CH₃ —CF₃ X83 (a and b) —CH₃ —CH₂CF₃  X84 (a and b) —CH₃ —OCF₃  X85 (a and b)—CH₃ —Cl  X86 (a and b) —CH₃ —Br  X87 (a and b) —CH₃ —I  X88 (a and b)—CH₃ -n-butyl  X89 (a and b) —CH₃ —CH₃  X90 (a and b) —CH₃ —SCF₃  X91 (aand b) —CH₃ —N(CH₂CH₃)₂  X92 (a and b) —CH₃ —OCF₂CHF₂  X93 (a and b)—CH₃ —C(OH)(CF₃)₂  X94 (a and b) —CH₃ -(1,1-dimethyl-pentyl)  X95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester  X96 (a and b) —CH₃—N-piperidinyl  X97 (a and b) —CF₃ —H  X98 (a and b) —CF₃ -tert-butyl X99 (a and b) —CF₃ -iso-butyl X100 (a and b) —CF₃ -sec-butyl X101 (aand b) —CF₃ -iso-propyl X102 (a and b) —CF₃ -n-propyl X103 (a and b)—CF₃ -cyclohexyl X104 (a and b) —CF₃ -tert-butoxy X105 (a and b) —CF₃-isopropoxy X106 (a and b) —CF₃ —CF₃ X107 (a and b) —CF₃ —CH₂CF₃ X108 (aand b) —CF₃ —OCF₃ X109 (a and b) —CF₃ —Cl X110 (a and b) —CF₃ —Br X111(a and b) —CF₃ —I X112 (a and b) —CF₃ -n-butyl X113 (a and b) —CF₃ —CH₃X114 (a and b) —CF₃ —SCF₃ X115 (a and b) —CF₃ —N(CH₂CH₃)₂ X116 (a and b)—CF₃ —OCF₂CHF₂ X117 (a and b) —CF₃ —C(OH)(CF₃)₂ X118 (a and b) —CF₃-(1,1-dimethyl-pentyl) X119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester X120 (a and b) —CF₃ —N-piperidinyl X121 (a and b) —CHF₂-tert-butyl X122 (a and b) —CHF₂ —H X123 (a and b) —CHF₂ -iso-butyl X124(a and b) —CHF₂ -sec-butyl X125 (a and b) —CHF₂ -iso-propyl X126 (a andb) —CHF₂ -n-propyl X127 (a and b) —CHF₂ -cyclohexyl X128 (a and b) —CHF₂-tert-butoxy X129 (a and b) —CHF₂ -isopropoxy X130 (a and b) —CHF₂ —CF₃X131 (a and b) —CHF₂ —CH₂CF₃ X132 (a and b) —CHF₂ —OCF₃ X133 (a and b)—CHF₂ —Cl X134 (a and b) —CHF₂ —Br X135 (a and b) —CHF₂ —I X136 (a andb) —CHF₂ -n-butyl X137 (a and b) —CHF₂ —CH₃ X138 (a and b) —CHF₂ —SCF₃X139 (a and b) —CHF₂ —N(CH₂CH₃)₂ X140 (a and b) —CHF₂ —OCF₂CHF₂ X141 (aand b) —CHF₂ —C(OH)(CF₃)₂ X142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)X143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester X144 (a andb) —CHF₂ —N-piperidinyl X145 (a and b) —OH —H X146 (a and b) —OH-tert-butyl X147 (a and b) —OH -iso-butyl X148 (a and b) —OH -sec-butylX149 (a and b) —OH -iso-propyl X150 (a and b) —OH -n-propyl X151 (a andb) —OH -cyclohexyl X152 (a and b) —OH -tert-butoxy X153 (a and b) —OH-isopropoxy X154 (a and b) —OH —CF₃ X155 (a and b) —OH —CH₂CF₃ X156 (aand b) —OH —OCF₃ X157 (a and b) —OH —Cl X158 (a and b) —OH —Br X159 (aand b) —OH —I X160 (a and b) —OH -n-butyl X161 (a and b) —OH —CH₃ X162(a and b) —OH —SCF₃ X163 (a and b) —OH —N(CH₂CH₃)₂ X164 (a and b) —OH—OCF₂CHF₂ X165 (a and b) —OH —C(OH)(CF₃)₂ X166 (a and b) —OH-(1,1-dimethyl-pentyl) X167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester X168 (a and b) —OH —N-piperidinyl X169 (a and b) —NO₂ —HX170 (a and b) —NO₂ -tert-butyl X171 (a and b) —NO₂ -iso-butyl X172 (aand b) —NO₂ -sec-butyl X173 (a and b) —NO₂ -iso-propyl X174 (a and b)—NO₂ -n-propyl X175 (a and b) —NO₂ -cyclohexyl X176 (a and b) —NO₂-tert-butoxy X177 (a and b) —NO₂ -isopropoxy X178 (a and b) —NO₂ —CF₃X179 (a and b) —NO₂ —CH₂CF₃ X180 (a and b) —NO₂ —OCF₃ X181 (a and b)—NO₂ —Cl X182 (a and b) —NO₂ —Br X183 (a and b) —NO₂ —I X184 (a and b)—NO₂ -n-butyl X185 (a and b) —NO₂ —CH₃ X186 (a and b) —NO₂ —SCF₃ X187 (aand b) —NO₂ —N(CH₂CH₃)₂ X188 (a and b) —NO₂ —OCF₂CHF₂ X189 (a and b)—NO₂ —C(OH)(CF₃)₂ X190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) X191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester X192 (a and b) —NO₂—N-piperidinyl X193 (a and b) —CN —H X194 (a and b) —CN -tert-butyl X195(a and b) —CN -iso-butyl X196 (a and b) —CN -sec-butyl X197 (a and b)—CN -iso-propyl X198 (a and b) —CN -n-propyl X199 (a and b) —CN-cyclohexyl X200 (a and b) —CN -tert-butoxy X201 (a and b) —CN-isopropoxy X202 (a and b) —CN —CF₃ X203 (a and b) —CN —CH₂CF₃ X204 (aand b) —CN —OCF₃ X205 (a and b) —CN —Cl X206 (a and b) —CN —Br X207 (aand b) —CN —I X208 (a and b) —CN -n-butyl X209 (a and b) —CN —CH₃ X210(a and b) —CN —SCF₃ X211 (a and b) —CN —N(CH₂CH₃)₂ X212 (a and b) —CN—OCF₂CHF₂ X213 (a and b) —CN —C(OH)(CF₃)₂ X214 (a and b) —CN-(1,1-dimethyl-pentyl) X215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester X216 (a and b) —CN —N-piperidinyl X217 (a and b) —Br —H X218(a and b) —Br -tert-butyl X219 (a and b) —Br -iso-butyl X220 (a and b)—Br -sec-butyl X221 (a and b) —Br -iso-propyl X222 (a and b) —Br-n-propyl X223 (a and b) —Br -cyclohexyl X224 (a and b) —Br -tert-butoxyX225 (a and b) —Br -isopropoxy X226 (a and b) —Br —CF₃ X227 (a and b)—Br —CH₂CF₃ X228 (a and b) —Br —OCF₃ X229 (a and b) —Br —Cl X230 (a andb) —Br —Br X231 (a and b) —Br —I X232 (a and b) —Br -n-butyl X233 (a andb) —Br —CH₃ X234 (a and b) —Br —SCF₃ X235 (a and b) —Br —N(CH₂CH₃)₂ X236(a and b) —Br —OCF₂CHF₂ X237 (a and b) —Br —C(OH)(CF₃)₂ X238 (a and b)—Br -(1,1-dimethyl-pentyl) X239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester X240 (a and b) —Br —N-piperidinyl X241 (a and b) —I-tert-butyl X242 (a and b) —I —H X243 (a and b) —I -iso-butyl X244 (aand b) —I -sec-butyl X245 (a and b) —I -iso-propyl X246 (a and b) —I-n-propyl X247 (a and b) —I -cyclohexyl X248 (a and b) —I -tert-butoxyX249 (a and b) —I -isopropoxy X250 (a and b) —I —CF₃ X251 (a and b) —I—CH₂CF₃ X252 (a and b) —I —OCF₃ X253 (a and b) —I —Cl X254 (a and b) —I—Br X255 (a and b) —I —I X256 (a and b) —I -n-butyl X257 (a and b) —I—CH₃ X258 (a and b) —I —SCF₃ X259 (a and b) —I —N(CH₂CH₃)₂ X260 (a andb) —I —OCF₂CHF₂ X261 (a and b) —I —C(OH)(CF₃)₂ X262 (a and b) —I-(1,1-dimethyl-pentyl) X263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester X264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 25 (Iy)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a)  Y1 (a and b) —H —H  Y2 (a and b) —H -tert-butyl  Y3 (a and b) —H-iso-butyl  Y4 (a and b) —H -sec-butyl  Y5 (a and b) —H -iso-propyl  Y6(a and b) —H -n-propyl  Y7 (a and b) —H -cyclohexyl  Y8 (a and b) —H-tert-butoxy  Y9 (a and b) —H -isopropoxy  Y10 (a and b) —H —CF₃  Y11 (aand b) —H —CH₂CF₃  Y12 (a and b) —H —OCF₃  Y13 (a and b) —H —Cl  Y14 (aand b) —H —Br  Y15 (a and b) —H —I  Y16 (a and b) —H -n-butyl  Y17 (aand b) —H —CH₃  Y18 (a and b) —H —SCF₃  Y19 (a and b) —H —N(CH₂CH₃)₂ Y20 (a and b) —H —OCF₂CHF₂  Y21 (a and b) —H —C(OH)(CF₃)₂  Y22 (a andb) —H -(1,1-dimethyl-pentyl)  Y23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester  Y24 (a and b) —H —N-piperidinyl  Y25 (a and b) —Cl —H Y26 (a and b) —Cl -tert-butyl  Y27 (a and b) —Cl -iso-butyl  Y28 (a andb) —Cl -sec-butyl  Y29 (a and b) —Cl -iso-propyl  Y30 (a and b) —Cl-n-propyl  Y31 (a and b) —Cl -cyclohexyl  Y32 (a and b) —Cl -tert-butoxy Y33 (a and b) —Cl -isopropoxy  Y34 (a and b) —Cl —CF₃  Y35 (a and b)—Cl —CH₂CF₃  Y36 (a and b) —Cl —OCF₃  Y37 (a and b) —Cl —Cl  Y38 (a andb) —Cl —Br  Y39 (a and b) —Cl —I  Y40 (a and b) —Cl -n-butyl  Y41 (a andb) —Cl —CH₃  Y42 (a and b) —Cl —SCF₃  Y43 (a and b) —Cl —N(CH₂CH₃)₂  Y44(a and b) —Cl —OCF₂CHF₂  Y45 (a and b) —Cl —C(OH)(CF₃)₂  Y46 (a and b)—Cl -(1,1-dimethyl-pentyl)  Y47 (a and b) —Cl -(1,1-dimethyl-aceticacid) ethyl ester  Y48 (a and b) —Cl —N-piperidinyl  Y49 (a and b) —F —H Y50 (a and b) —F -tert-butyl  Y51 (a and b) —F -iso-butyl  Y52 (a andb) —F -sec-butyl  Y53 (a and b) —F -iso-propyl  Y54 (a and b) —F-n-propyl  Y55 (a and b) —F -cyclohexyl  Y56 (a and b) —F -tert-butoxy Y57 (a and b) —F -isopropoxy  Y58 (a and b) —F —CF₃  Y59 (a and b) —F—CH₂CF₃  Y60 (a and b) —F —OCF₃  Y61 (a and b) —F —Cl  Y62 (a and b) —F—Br  Y63 (a and b) —F —I  Y64 (a and b) —F -n-butyl  Y65 (a and b) —F—CH₃  Y66 (a and b) —F —SCF₃  Y67 (a and b) —F —N(CH₂CH₃)₂  Y68 (a andb) —F —OCF₂CHF₂  Y69 (a and b) —F —C(OH)(CF₃)₂  Y70 (a and b) —F-(1,1-dimethyl-pentyl)  Y71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester  Y72 (a and b) —F —N-piperidinyl  Y73 (a and b) —CH₃ —H  Y74(a and b) —CH₃ -iso-butyl  Y75 (a and b) —CH₃ -tert-butyl  Y76 (a and b)—CH₃ -sec-butyl  Y77 (a and b) —CH₃ -iso-propyl  Y78 (a and b) —CH₃-n-propyl  Y79 (a and b) —CH₃ -cyclohexyl  Y80 (a and b) —CH₃-tert-butoxy  Y81 (a and b) —CH₃ -isopropoxy  Y82 (a and b) —CH₃ —CF₃ Y83 (a and b) —CH₃ —CH₂CF₃  Y84 (a and b) —CH₃ —OCF₃  Y85 (a and b)—CH₃ —Cl  Y86 (a and b) —CH₃ —Br  Y87 (a and b) —CH₃ —I  Y88 (a and b)—CH₃ -n-butyl  Y89 (a and b) —CH₃ —CH₃  Y90 (a and b) —CH₃ —SCF₃  Y91 (aand b) —CH₃ —N(CH₂CH₃)₂  Y92 (a and b) —CH₃ —OCF₂CHF₂  Y93 (a and b)—CH₃ —C(OH)(CF₃)₂  Y94 (a and b) —CH₃ -(1,1-dimethyl-pentyl)  Y95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester  Y96 (a and b) —CH₃—N-piperidinyl  Y97 (a and b) —CF₃ —H  Y98 (a and b) —CF₃ -tert-butyl Y99 (a and b) —CF₃ -iso-butyl Y100 (a and b) —CF₃ -sec-butyl Y101 (aand b) —CF₃ -iso-propyl Y102 (a and b) —CF₃ -n-propyl Y103 (a and b)—CF₃ -cyclohexyl Y104 (a and b) —CF₃ -tert-butoxy Y105 (a and b) —CF₃-isopropoxy Y106 (a and b) —CF₃ —CF₃ Y107 (a and b) —CF₃ —CH₂CF₃ Y108 (aand b) —CF₃ —OCF₃ Y109 (a and b) —CF₃ —Cl Y110 (a and b) —CF₃ —Br Y111(a and b) —CF₃ —I Y112 (a and b) —CF₃ -n-butyl Y113 (a and b) —CF₃ —CH₃Y114 (a and b) —CF₃ —SCF₃ Y115 (a and b) —CF₃ —N(CH₂CH₃)₂ Y116 (a and b)—CF₃ —OCF₂CHF₂ Y117 (a and b) —CF₃ —C(OH)(CF₃)₂ Y118 (a and b) —CF₃-(1,1-dimethyl-pentyl) Y119 (a and b) —CF₃ -(1,1-dimethyl-acetic acid)ethyl ester Y120 (a and b) —CF₃ —N-piperidinyl Y121 (a and b) —CHF₂-tert-butyl Y122 (a and b) —CHF₂ —H Y123 (a and b) —CHF₂ -iso-butyl Y124(a and b) —CHF₂ -sec-butyl Y125 (a and b) —CHF₂ -iso-propyl Y126 (a andb) —CHF₂ -n-propyl Y127 (a and b) —CHF₂ -cyclohexyl Y128 (a and b) —CHF₂-tert-butoxy Y129 (a and b) —CHF₂ -isopropoxy Y130 (a and b) —CHF₂ —CF₃Y131 (a and b) —CHF₂ —CH₂CF₃ Y132 (a and b) —CHF₂ —OCF₃ Y133 (a and b)—CHF₂ —Cl Y134 (a and b) —CHF₂ —Br Y135 (a and b) —CHF₂ —I Y136 (a andb) —CHF₂ -n-butyl Y137 (a and b) —CHF₂ —CH₃ Y138 (a and b) —CHF₂ —SCF₃Y139 (a and b) —CHF₂ —N(CH₂CH₃)₂ Y140 (a and b) —CHF₂ —OCF₂CHF₂ Y141 (aand b) —CHF₂ —C(OH)(CF₃)₂ Y142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl)Y143 (a and b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester Y144 (a andb) —CHF₂ —N-piperidinyl Y145 (a and b) —OH —H Y146 (a and b) —OH-tert-butyl Y147 (a and b) —OH -iso-butyl Y148 (a and b) —OH -sec-butylY149 (a and b) —OH -iso-propyl Y150 (a and b) —OH -n-propyl Y151 (a andb) —OH -cyclohexyl Y152 (a and b) —OH -tert-butoxy Y153 (a and b) —OH-isopropoxy Y154 (a and b) —OH —CF₃ Y155 (a and b) —OH —CH₂CF₃ Y156 (aand b) —OH —OCF₃ Y157 (a and b) —OH —Cl Y158 (a and b) —OH —Br Y159 (aand b) —OH —I Y160 (a and b) —OH -n-butyl Y161 (a and b) —OH —CH₃ Y162(a and b) —OH —SCF₃ Y163 (a and b) —OH —N(CH₂CH₃)₂ Y164 (a and b) —OH—OCF₂CHF₂ Y165 (a and b) —OH —C(OH)(CF₃)₂ Y166 (a and b) —OH-(1,1-dimethyl-pentyl) Y167 (a and b) —OH -(1,1-dimethyl-acetic acid)ethyl ester Y168 (a and b) —OH —N-piperidinyl Y169 (a and b) —NO₂ —HY170 (a and b) —NO₂ -tert-butyl Y171 (a and b) —NO₂ -iso-butyl Y172 (aand b) —NO₂ -sec-butyl Y173 (a and b) —NO₂ -iso-propyl Y174 (a and b)—NO₂ -n-propyl Y175 (a and b) —NO₂ -cyclohexyl Y176 (a and b) —NO₂-tert-butoxy Y177 (a and b) —NO₂ -isopropoxy Y178 (a and b) —NO₂ —CF₃Y179 (a and b) —NO₂ —CH₂CF₃ Y180 (a and b) —NO₂ —OCF₃ Y181 (a and b)—NO₂ —Cl Y182 (a and b) —NO₂ —Br Y183 (a and b) —NO₂ —I Y184 (a and b)—NO₂ -n-butyl Y185 (a and b) —NO₂ —CH₃ Y186 (a and b) —NO₂ —SCF₃ Y187 (aand b) —NO₂ —N(CH₂CH₃)₂ Y188 (a and b) —NO₂ —OCF₂CHF₂ Y189 (a and b)—NO₂ —C(OH)(CF₃)₂ Y190 (a and b) —NO₂ -(1,1-dimethyl-pentyl) Y191 (a andb) —NO₂ -(1,1-dimethyl-acetic acid) ethyl ester Y192 (a and b) —NO₂—N-piperidinyl Y193 (a and b) —CN —H Y194 (a and b) —CN -tert-butyl Y195(a and b) —CN -iso-butyl Y196 (a and b) —CN -sec-butyl Y197 (a and b)—CN -iso-propyl Y198 (a and b) —CN -n-propyl Y199 (a and b) —CN-cyclohexyl Y200 (a and b) —CN -tert-butoxy Y201 (a and b) —CN-isopropoxy Y202 (a and b) —CN —CF₃ Y203 (a and b) —CN —CH₂CF₃ Y204 (aand b) —CN —OCF₃ Y205 (a and b) —CN —Cl Y206 (a and b) —CN —Br Y207 (aand b) —CN —I Y208 (a and b) —CN -n-butyl Y209 (a and b) —CN —CH₃ Y210(a and b) —CN —SCF₃ Y211 (a and b) —CN —N(CH₂CH₃)₂ Y212 (a and b) —CN—OCF₂CHF₂ Y213 (a and b) —CN —C(OH)(CF₃)₂ Y214 (a and b) —CN-(1,1-dimethyl-pentyl) Y215 (a and b) —CN -(1,1-dimethyl-acetic acid)ethyl ester Y216 (a and b) —CN —N-piperidinyl Y217 (a and b) —Br —H Y218(a and b) —Br -tert-butyl Y219 (a and b) —Br -iso-butyl Y220 (a and b)—Br -sec-butyl Y221 (a and b) —Br -iso-propyl Y222 (a and b) —Br-n-propyl Y223 (a and b) —Br -cyclohexyl Y224 (a and b) —Br -tert-butoxyY225 (a and b) —Br -isopropoxy Y226 (a and b) —Br —CF₃ Y227 (a and b)—Br —CH₂CF₃ Y228 (a and b) —Br —OCF₃ Y229 (a and b) —Br —Cl Y230 (a andb) —Br —Br Y231 (a and b) —Br —I Y232 (a and b) —Br -n-butyl Y233 (a andb) —Br —CH₃ Y234 (a and b) —Br —SCF₃ Y235 (a and b) —Br —N(CH₂CH₃)₂ Y236(a and b) —Br —OCF₂CHF₂ Y237 (a and b) —Br —C(OH)(CF₃)₂ Y238 (a and b)—Br -(1,1-dimethyl-pentyl) Y239 (a and b) —Br -(1,1-dimethyl-aceticacid) ethyl ester Y240 (a and b) —Br —N-piperidinyl Y241 (a and b) —I-tert-butyl Y242 (a and b) —I —H Y243 (a and b) —I -iso-butyl Y244 (aand b) —I -sec-butyl Y245 (a and b) —I -iso-propyl Y246 (a and b) —I-n-propyl Y247 (a and b) —I -cyclohexyl Y248 (a and b) —I -tert-butoxyY249 (a and b) —I -isopropoxy Y250 (a and b) —I —CF₃ Y251 (a and b) —I—CH₂CF₃ Y252 (a and b) —I —OCF₃ Y253 (a and b) —I —Cl Y254 (a and b) —I—Br Y255 (a and b) —I —I Y256 (a and b) —I -n-butyl Y257 (a and b) —I—CH₃ Y258 (a and b) —I —SCF₃ Y259 (a and b) —I —N(CH₂CH₃)₂ Y260 (a andb) —I —OCF₂CHF₂ Y261 (a and b) —I —C(OH)(CF₃)₂ Y262 (a and b) —I-(1,1-dimethyl-pentyl) Y263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester Y264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 26 (Iz)

and pharmaceutically acceptable salts thereof, wherein: Compound Y R₁(R₈)_(a) (R₈)_(b)  Z1 (a and b) S —H —Cl —H  Z2 (a and b) S —H —Br —H Z3 (a and b) S —H —F —H  Z4 (a and b) S —H —CH₃ —H  Z5 (a and b) S —H—CF₃ —H  Z6 (a and b) S —H —OCH₃ —H  Z7 (a and b) S —H —OCH₂CH₃ —H  Z8(a and b) S —H —OCF₃ —H  Z9 (a and b) S —H -tert-butyl —H  Z10 (a and b)S —H -iso-propyl —H  Z11 (a and b) S —H —CH₃ —CH₃  Z12 (a and b) S —H —H—H  Z13 (a and b) S —H —H —Cl  Z14 (a and b) S —H —H —Br  Z15 (a and b)S —H —H —F  Z16 (a and b) S —H —H —CH₃  Z17 (a and b) S —H —H —CF₃  Z18(a and b) S —H —H —OCH₃  Z19 (a and b) S —H —H —OCH₂CH₃  Z20 (a and b) S—H —H —OCF₃  Z21 (a and b) S —H —H -tert-butyl  Z22 (a and b) S —H —H-iso-propyl  Z23 (a and b) S —Cl —Cl —H  Z24 (a and b) S —Cl —Br —H  Z25(a and b) S —Cl —F —H  Z26 (a and b) S —Cl —CH₃ —H  Z27 (a and b) S —Cl—CF₃ —H  Z28 (a and b) S —Cl —OCH₃ —H  Z29 (a and b) S —Cl —OCH₂CH₃ —H Z30 (a and b) S —Cl —OCF₃ —H  Z31 (a and b) S —Cl -tert-butyl —H  Z32(a and b) S —Cl -iso-propyl —H  Z33 (a and b) S —Cl —CH₃ —CH₃  Z34 (aand b) S —Cl —H —H  Z35 (a and b) S —Cl —H —Cl  Z36 (a and b) S —Cl —H—Br  Z37 (a and b) S —Cl —H —F  Z38 (a and b) S —Cl —H —CH₃  Z39 (a andb) S —Cl —H —CF₃  Z40 (a and b) S —Cl —H —OCH₃  Z41 (a and b) S —Cl —H—OCH₂CH₃  Z42 (a and b) S —Cl —H —OCF₃  Z43 (a and b) S —Cl —H-tert-butyl  Z44 (a and b) S —Cl —H -iso-propyl  Z45 (a and b) S —Cl —H—OCF₃  Z46 (a and b) S —Cl —H -tert-butyl  Z47 (a and b) S —Cl —H-iso-propyl  Z48 (a and b) S —CH₃ —Cl —H  Z49 (a and b) S —CH₃ —Br —H Z50 (a and b) S —CH₃ —F —H  Z51 (a and b) S —CH₃ —CH₃ —H  Z52 (a and b)S —CH₃ —CF₃ —H  Z53 (a and b) S —CH₃ —OCH₃ —H  Z54 (a and b) S —CH₃—OCH₂CH₃ —H  Z55 (a and b) S —CH₃ —OCF₃ —H  Z56 (a and b) S —CH₃-tert-butyl —H  Z57 (a and b) S —CH₃ -iso-propyl —H  Z58 (a and b) S—CH₃ —CH₃ —CH₃  Z59 (a and b) S —CH₃ —H —H  Z60 (a and b) S —CH₃ —H —Cl Z61 (a and b) S —CH₃ —H —Br  Z62 (a and b) S —CH₃ —H —F  Z63 (a and b)S —CH₃ —H —CH₃  Z64 (a and b) S —CH₃ —H —CF₃  Z65 (a and b) S —CH₃ —H—OCH₃  Z66 (a and b) S —CH₃ —H —OCH₂CH₃  Z67 (a and b) S —CH₃ —H —OCF₃ Z68 (a and b) S —CH₃ —H -tert-butyl  Z69 (a and b) S —CH₃ —H-iso-propyl  Z70 (a and b) S —CF₃ —Cl —H  Z71 (a and b) S —CF₃ —Br —H Z72 (a and b) S —CF₃ —F —H  Z73 (a and b) S —CF₃ —CH₃ —H  Z74 (a and b)S —CF₃ —CF₃ —H  Z75 (a and b) S —CF₃ —OCH₃ —H  Z76 (a and b) S —CF₃—OCH₂CH₃ —H  Z77 (a and b) S —CF₃ —OCF₃ —H  Z78 (a and b) S —CF₃-tert-butyl —H  Z79 (a and b) S —CF₃ -iso-propyl —H  Z80 (a and b) S—CF₃ —CH₃ —CH₃  Z81 (a and b) S —CF₃ —H —H  Z82 (a and b) S —CF₃ —H —Cl Z83 (a and b) S —CF₃ —H —Br  Z84 (a and b) S —CF₃ —H —F  Z85 (a and b)S —CF₃ —H —CH₃  Z86 (a and b) S —CF₃ —H —CF₃  Z87 (a and b) S —CF₃ —H—OCH₃  Z88 (a and b) S —CF₃ —H —OCH₂CH₃  Z89 (a and b) S —CF₃ —H —OCF₃ Z90 (a and b) S —CF₃ —H -tert-butyl  Z91 (a and b) S —CF₃ —H-iso-propyl  Z92 (a and b) S —CHF₂ —Cl —H  Z93 (a and b) S —CHF₂ —Br —H Z94 (a and b) S —CHF₂ —F —H  Z95 (a and b) S —CHF₂ —CH₃ —H  Z96 (a andb) S —CHF₂ —CF₃ —H  Z97 (a and b) S —CHF₂ —OCH₃ —H  Z98 (a and b) S—CHF₂ —OCH₂CH₃ —H  Z99 (a and b) S —CHF₂ —OCF₃ —H Z100 (a and b) S —CHF₂-tert-butyl —H Z101 (a and b) S —CHF₂ -iso-propyl —H Z102 (a and b) S—CHF₂ —CH₃ —CH₃ Z103 (a and b) S —CHF₂ —H —H Z104 (a and b) S —CHF₂ —H—Cl Z105 (a and b) S —CHF₂ —H —Br Z106 (a and b) S —CHF₂ —H —F Z107 (aand b) S —CHF₂ —H —CH₃ Z108 (a and b) S —CHF₂ —H —CF₃ Z109 (a and b) S—CHF₂ —H —OCH₃ Z110 (a and b) S —CHF₂ —H —OCH₂CH₃ Z111 (a and b) S —CHF₂—H —OCF₃ Z112 (a and b) S —CHF₂ —H -tert-butyl Z113 (a and b) S —CHF₂ —H-iso-propyl Z114 (a and b) S —OH —Cl —H Z115 (a and b) S —OH —Br —H Z116(a and b) S —OH —F —H Z117 (a and b) S —OH —CH₃ —H Z118 (a and b) S —OH—CF₃ —H Z119 (a and b) S —OH —OCH₃ —H Z120 (a and b) S —OH —OCH₂CH₃ —HZ121 (a and b) S —OH —OCF₃ —H Z122 (a and b) S —OH -tert-butyl —H Z123(a and b) S —OH -iso-propyl —H Z124 (a and b) S —OH —CH₃ —CH₃ Z125 (aand b) S —OH —H —H Z126 (a and b) S —OH —H —Cl Z127 (a and b) S —OH —H—Br Z128 (a and b) S —OH —H —F Z129 (a and b) S —OH —H —CH₃ Z130 (a andb) S —OH —H —CF₃ Z131 (a and b) S —OH —H —OCH₃ Z132 (a and b) S —OH —H—OCH₂CH₃ Z133 (a and b) S —OH —H —OCF₃ Z134 (a and b) S —OH —H-tert-butyl Z135 (a and b) S —OH —H -iso-propyl Z136 (a and b) S —NO₂—Cl —H Z137 (a and b) S —NO₂ —Br —H Z138 (a and b) S —NO₂ —F —H Z139 (aand b) S —NO₂ —CH₃ —H Z140 (a and b) S —NO₂ —CF₃ —H Z141 (a and b) S—NO₂ —OCH₃ —H Z142 (a and b) S —NO₂ —OCH₂CH₃ —H Z143 (a and b) S —NO₂—OCF₃ —H Z144 (a and b) S —NO₂ -tert-butyl —H Z145 (a and b) S —NO₂-iso-propyl —H Z146 (a and b) S —NO₂ —CH₃ —CH₃ Z147 (a and b) S —NO₂ —H—H Z148 (a and b) S —NO₂ —H —Cl Z149 (a and b) S —NO₂ —H —Br Z150 (a andb) S —NO₂ —H —F Z151 (a and b) S —NO₂ —H —CH₃ Z152 (a and b) S —NO₂ —H—CF₃ Z153 (a and b) S —NO₂ —H —OCH₃ Z154 (a and b) S —NO₂ —H —OCH₂CH₃Z155 (a and b) S —NO₂ —H —OCF₃ Z156 (a and b) S —NO₂ —H -tert-butyl Z157(a and b) S —NO₂ —H -iso-propyl Z158 (a and b) S —CN —Br —H Z159 (a andb) S —CN —Cl —H Z160 (a and b) S —CN —F —H Z161 (a and b) S —CN —CH₃ —HZ162 (a and b) S —CN —CF₃ —H Z163 (a and b) S —CN —OCH₃ —H Z164 (a andb) S —CN —OCH₂CH₃ —H Z165 (a and b) S —CN —OCF₃ —H Z166 (a and b) S —CN-tert-butyl —H Z167 (a and b) S —CN -iso-propyl —H Z168 (a and b) S —CN—CH₃ —CH₃ Z169 (a and b) S —CN —H —H Z170 (a and b) S —CN —H —Cl Z171 (aand b) S —CN —H —Br Z172 (a and b) S —CN —H —F Z173 (a and b) S —CN —H—CH₃ Z174 (a and b) S —CN —H —CF₃ Z175 (a and b) S —CN —H —OCH₃ Z176 (aand b) S —CN —H —OCH₂CH₃ Z177 (a and b) S —CN —H —OCF₃ Z178 (a and b) S—CN —H -tert-butyl Z179 (a and b) S —CN —H -iso-propyl Z180 (a and b) S—Br —Br —H Z181 (a and b) S —Br —Cl —H Z182 (a and b) S —Br —F —H Z183(a and b) S —Br —CH₃ —H Z184 (a and b) S —Br —CF₃ —H Z185 (a and b) S—Br —OCH₃ —H Z186 (a and b) S —Br —OCH₂CH₃ —H Z187 (a and b) S —Br —OCF₃—H Z188 (a and b) S —Br -tert-butyl —H Z189 (a and b) S —Br -iso-propyl—H Z190 (a and b) S —Br —CH₃ —CH₃ Z191 (a and b) S —Br —H —H Z192 (a andb) S —Br —H —Cl Z193 (a and b) S —Br —H —Br Z194 (a and b) S —Br —H —FZ195 (a and b) S —Br —H —CH₃ Z196 (a and b) S —Br —H —CF₃ Z197 (a and b)S —Br —H —OCH₃ Z198 (a and b) S —Br —H —OCH₂CH₃ Z199 (a and b) S —Br —H—OCF₃ Z200 (a and b) S —Br —H -tert-butyl Z201 (a and b) S —Br —H-iso-propyl Z202 (a and b) S —I —Cl —H Z203 (a and b) S —I —Br —H Z204(a and b) S —I —F —H Z205 (a and b) S —I —CH₃ —H Z206 (a and b) S —I—CF₃ —H Z207 (a and b) S —I —OCH₃ —H Z208 (a and b) S —I —OCH₂CH₃ —HZ209 (a and b) S —I —OCF₃ —H Z210 (a and b) S —I -tert-butyl —H Z211 (aand b) S —I -iso-propyl —H Z212 (a and b) S —I —CH₃ —CH₃ Z213 (a and b)S —I —H —H Z214 (a and b) S —I —H —Cl Z215 (a and b) S —I —H —Br Z216 (aand b) S —I —H —F Z217 (a and b) S —I —H —CH₃ Z218 (a and b) S —I —H—CF₃ Z219 (a and b) S —I —H —OCH₃ Z220 (a and b) S —I —H —OCH₂CH₃ Z221(a and b) S —I —H —OCF₃ Z222 (a and b) S —I —H -tert-butyl Z223 (a andb) S —I —H -iso-propyl Z224 (a and b) O —H —Cl —H Z225 (a and b) O —H—Br —H Z226 (a and b) O —H —F —H Z227 (a and b) O —H —CH₃ —H Z228 (a andb) O —H —CF₃ —H Z229 (a and b) O —H —OCH₃ —H Z230 (a and b) O —H—OCH₂CH₃ —H Z231 (a and b) O —H —OCF₃ —H Z232 (a and b) O —H -tert-butyl—H Z233 (a and b) O —H -iso-propyl —H Z234 (a and b) O —H —CH₃ —CH₃ Z235(a and b) O —H —H —H Z236 (a and b) O —H —H —Cl Z237 (a and b) O —H —H—Br Z238 (a and b) O —H —H —F Z239 (a and b) O —H —H —CH₃ Z240 (a and b)O —H —H —CF₃ Z241 (a and b) O —H —H —OCH₃ Z242 (a and b) O —H —H—OCH₂CH₃ Z243 (a and b) O —H —H —OCF₃ Z244 (a and b) O —H —H -tert-butylZ245 (a and b) O —H —H -iso-propyl Z246 (a and b) O —Cl —Cl —H Z247 (aand b) O —Cl —Br —H Z248 (a and b) O —Cl —F —H Z249 (a and b) O —Cl —CH₃—H Z250 (a and b) O —Cl —CF₃ —H Z251 (a and b) O —Cl —OCH₃ —H Z252 (aand b) O —Cl —OCH₂CH₃ —H Z253 (a and b) O —Cl —OCF₃ —H Z254 (a and b) O—Cl -tert-butyl —H Z255 (a and b) O —Cl -iso-propyl —H Z256 (a and b) O—Cl —CH₃ —CH₃ Z257 (a and b) O —Cl —H —H Z258 (a and b) O —Cl —H —CH₃Z259 (a and b) O —Cl —H —Cl Z260 (a and b) O —Cl —H —Br Z261 (a and b) O—Cl —H —F Z262 (a and b) O —Cl —H —CF₃ Z263 (a and b) O —Cl —H —OCH₃Z264 (a and b) O —Cl —H —OCH₂CH₃ Z265 (a and b) O —Cl —H —OCF₃ Z266 (aand b) O —Cl —H -tert-butyl Z267 (a and b) O —Cl —H -iso-propyl Z268 (aand b) O —Cl —H —OCF₃ Z269 (a and b) O —Cl —H -tert-butyl Z270 (a and b)O —Cl —H -iso-propyl Z271 (a and b) O —CH₃ —Cl —H Z272 (a and b) O —CH₃—Br —H Z273 (a and b) O —CH₃ —F —H Z274 (a and b) O —CH₃ —CH₃ —H Z275 (aand b) O —CH₃ —CF₃ —H Z276 (a and b) O —CH₃ —OCH₃ —H Z277 (a and b) O—CH₃ —OCH₂CH₃ —H Z278 (a and b) O —CH₃ —OCF₃ —H Z279 (a and b) O —CH₃-tert-butyl —H Z280 (a and b) O —CH₃ -iso-propyl —H Z281 (a and b) O—CH₃ —CH₃ —CH₃ Z282 (a and b) O —CH₃ —H —H Z283 (a and b) O —CH₃ —H —ClZ284 (a and b) O —CH₃ —H —Br Z285 (a and b) O —CH₃ —H —F Z286 (a and b)O —CH₃ —H —CH₃ Z287 (a and b) O —CH₃ —H —CF₃ Z288 (a and b) O —CH₃ —H—OCH₃ Z289 (a and b) O —CH₃ —H —OCH₂CH₃ Z290 (a and b) O —CH₃ —H —OCF₃Z291 (a and b) O —CH₃ —H -tert-butyl Z292 (a and b) O —CH₃ —H-iso-propyl Z293 (a and b) O —CF₃ —Cl —H Z294 (a and b) O —CF₃ —Br —HZ295 (a and b) O —CF₃ —F —H Z296 (a and b) O —CF₃ —CH₃ —H Z297 (a and b)O —CF₃ —CF₃ —H Z298 (a and b) O —CF₃ —OCH₃ —H Z299 (a and b) O —CF₃—OCH₂CH₃ —H Z300 (a and b) O —CF₃ —OCF₃ —H Z301 (a and b) O —CF₃-tert-butyl —H Z302 (a and b) O —CF₃ -iso-propyl —H Z303 (a and b) O—CF₃ —CH₃ —CH₃ Z304 (a and b) O —CF₃ —H —H Z305 (a and b) O —CF₃ —H —ClZ306 (a and b) O —CF₃ —H —Br Z307 (a and b) O —CF₃ —H —F Z308 (a and b)O —CF₃ —H —CH₃ Z309 (a and b) O —CF₃ —H —CF₃ Z310 (a and b) O —CF₃ —H—OCH₃ Z311 (a and b) O —CF₃ —H —OCH₂CH₃ Z312 (a and b) O —CF₃ —H —OCF₃Z313 (a and b) O —CF₃ —H -tert-butyl Z314 (a and b) O —CF₃ —H-iso-propyl Z315 (a and b) O —CHF₂ —Cl —H Z316 (a and b) O —CHF₂ —Br —HZ317 (a and b) O —CHF₂ —F —H Z318 (a and b) O —CHF₂ —CH₃ —H Z319 (a andb) O —CHF₂ —CF₃ —H Z320 (a and b) O —CHF₂ —OCH₃ —H Z321 (a and b) O—CHF₂ —OCH₂CH₃ —H Z322 (a and b) O —CHF₂ —OCF₃ —H Z323 (a and b) O —CHF₂-tert-butyl —H Z324 (a and b) O —CHF₂ -iso-propyl —H Z325 (a and b) O—CHF₂ —CH₃ —CH₃ Z326 (a and b) O —CHF₂ —H —H Z327 (a and b) O —CHF₂ —H—Cl Z328 (a and b) O —CHF₂ —H —Br Z329 (a and b) O —CHF₂ —H —F Z330 (aand b) O —CHF₂ —H —CH₃ Z331 (a and b) O —CHF₂ —H —CF₃ Z332 (a and b) O—CHF₂ —H —OCH₃ Z333 (a and b) O —CHF₂ —H —OCH₂CH₃ Z334 (a and b) O —CHF₂—H —OCF₃ Z335 (a and b) O —CHF₂ —H -tert-butyl Z336 (a and b) O —CHF₂ —H-iso-propyl Z337 (a and b) O —OH —Cl —H Z338 (a and b) O —OH —Br —IIZ339 (a and b) O —OH —F —H Z340 (a and b) O —OH —CH₃ —H Z341 (a and b) O—OH —CF₃ —H Z342 (a and b) O —OH —OCH₃ —H Z343 (a and b) O —OH —OCH₂CH₃—H Z344 (a and b) O —OH —OCF₃ —H Z345 (a and b) O —OH -tert-butyl —HZ346 (a and b) O —OH -iso-propyl —H Z347 (a and b) O —OH —CH₃ —CH₃ Z348(a and b) O —OH —H —H Z349 (a and b) O —OH —H —Cl Z350 (a and b) O —OH—H —Br Z351 (a and b) O —OH —H —F Z352 (a and b) O —OH —H —CH₃ Z353 (aand b) O —OH —H —CF₃ Z354 (a and b) O —OH —H —OCH₃ Z355 (a and b) O —OH—H —OCH₂CH₃ Z356 (a and b) O —OH —H —OCF₃ Z357 (a and b) O —OH —H-tert-butyl Z358 (a and b) O —OH —H -iso-propyl Z359 (a and b) O —NO₂—Cl —H Z360 (a and b) O —NO₂ —Br —H Z361 (a and b) O —NO₂ —F —H Z362 (aand b) O —NO₂ —CH₃ —H Z363 (a and b) O —NO₂ —CF₃ —H Z364 (a and b) O—NO₂ —OCH₃ —H Z365 (a and b) O —NO₂ —OCH₂CH₃ —H Z366 (a and b) O —NO₂—OCF₃ —H Z367 (a and b) O —NO₂ -tert-butyl —H Z368 (a and b) O —NO₂-iso-propyl —H Z369 (a and b) O —NO₂ —CH₃ —CH₃ Z370 (a and b) O —NO₂ —H—H Z371 (a and b) O —NO₂ —H —Cl Z372 (a and b) O —NO₂ —H —Br Z373 (a andb) O —NO₂ —H —F Z374 (a and b) O —NO₂ —H —CH₃ Z375 (a and b) O —NO₂ —H—CF₃ Z376 (a and b) O —NO₂ —H —OCH₃ Z377 (a and b) O —NO₂ —H —OCH₂CH₃Z378 (a and b) O —NO₂ —H —OCF₃ Z379 (a and b) O —NO₂ —H -tert-butyl Z380(a and b) O —NO₂ —H -iso-propyl Z381 (a and b) O —CN —Br —H Z382 (a andb) O —CN —Cl —H Z383 (a and b) O —CN —F —H Z384 (a and b) O —CN —CH₃ —HZ385 (a and b) O —CN —CF₃ —H Z386 (a and b) O —CN —OCH₃ —H Z387 (a andb) O —CN —OCH₂CH₃ —H Z388 (a and b) O —CN —OCF₃ —H Z389 (a and b) O —CN-tert-butyl —H Z390 (a and b) O —CN -iso-propyl —H Z391 (a and b) O —CN—CH₃ —CH₃ Z392 (a and b) O —CN —H —H Z393 (a and b) O —CN —H —Cl Z394 (aand b) O —CN —H —Br Z395 (a and b) O —CN —H —F Z396 (a and b) O —CN —H—CH₃ Z397 (a and b) O —CN —H —CF₃ Z398 (a and b) O —CN —H —OCH₃ Z399 (aand b) O —CN —H —OCH₂CH₃ Z400 (a and b) O —CN —H —OCF₃ Z401 (a and b) O—CN —H -tert-butyl Z402 (a and b) O —CN —H -iso-propyl Z403 (a and b) O—Br —Br —H Z404 (a and b) O —Br —Cl —H Z405 (a and b) O —Br —F —H Z406(a and b) O —Br —CH₃ —H Z407 (a and b) O —Br —CF₃ —H Z408 (a and b) O—Br —OCH₃ —H Z409 (a and b) O —Br —OCH₂CH₃ —H Z410 (a and b) O —Br —OCF₃—H Z411 (a and b) O —Br -tert-butyl —H Z412 (a and b) O —Br -iso-propyl—H Z413 (a and b) O —Br —CH₃ —CH₃ Z414 (a and b) O —Br —H —H Z415 (a andb) O —Br —H —Cl Z416 (a and b) O —Br —H —Br Z417 (a and b) O —Br —H —FZ418 (a and b) O —Br —H —CH₃ Z419 (a and b) O —Br —H —CF₃ Z420 (a and b)O —Br —H —OCH₃ Z421 (a and b) O —Br —H —OCH₂CH₃ Z422 (a and b) O —Br —H—OCF₃ Z423 (a and b) O —Br —H -tert-butyl Z424 (a and b) O —Br —H-iso-propyl Z425 (a and b) O —I —Cl —H Z426 (a and b) O —I —Br —H Z427(a and b) O —I —F —H Z428 (a and b) O —I —CH₃ —H Z429 (a and b) O —I—CF₃ —H Z430 (a and b) O —I —OCH₃ —H Z431 (a and b) O —I —OCH₂CH₃ —HZ432 (a and b) O —I —OCF₃ —H Z433 (a and b) O —I -tert-butyl —H Z434 (aand b) O —I -iso-propyl —H Z435 (a and b) O —I —CH₃ —CH₃ Z436 (a and b)O —I —H —H Z437 (a and b) O —I —H —Cl Z438 (a and b) O —I —H —Br Z439 (aand b) O —I —H —F Z440 (a and b) O —I —H —CH₃ Z441 (a and b) O —I —H—CF₃ Z442 (a and b) O —I —H —OCH₃ Z443 (a and b) O —I —H —OCH₂CH₃ Z444(a and b) O —I —H —OCF₃ Z445 (a and b) O —I —H -tert-butyl Z446 (a andb) O —I —H -iso-propyl Z447 (a and b) NH —H —Cl —H Z448 (a and b) NH —H—Br —H Z449 (a and b) NH —H —F —H Z450 (a and b) NH —H —CH₃ —H Z451 (aand b) NH —H —CF₃ —H Z452 (a and b) NH —H —OCH₃ —H Z453 (a and b) NH —H—OCH₂CH₃ —H Z454 (a and b) NH —H —OCF₃ —H Z455 (a and b) NH —H-tert-butyl —H Z456 (a and b) NH —H -iso-propyl —H Z457 (a and b) NH —H—CH₃ —CH₃ Z458 (a and b) NH —H —H —H Z459 (a and b) NH —H —H —Cl Z460 (aand b) NH —H —H —Br Z461 (a and b) NH —H —H —F Z462 (a and b) NH —H —H—CH₃ Z463 (a and b) NH —H —H —CF₃ Z464 (a and b) NH —H —H —OCH₃ Z465 (aand b) NH —H —H —OCH₂CH₃ Z466 (a and b) NH —H —H —OCF₃ Z467 (a and b) NH—H —H -tert-butyl Z468 (a and b) NH —H —H -iso-propyl Z469 (a and b) NH—Cl —Cl —H Z470 (a and b) NH —Cl —Br —H Z471 (a and b) NH —Cl —F —H Z472(a and b) NH —Cl —CH₃ —H Z473 (a and b) NH —Cl —CF₃ —H Z474 (a and b) NH—Cl —OCH₃ —H Z475 (a and b) NH —Cl —OCH₂CH₃ —H Z476 (a and b) NH —Cl—OCF₃ —H Z477 (a and b) NH —Cl -tert-butyl —H Z478 (a and b) NH —Cl-iso-propyl —H Z479 (a and b) NH —Cl —CH₃ —CH₃ Z480 (a and b) NH —Cl —H—H Z481 (a and b) NH —Cl —H —CH₃ Z482 (a and b) NH —Cl —H —Cl Z483 (aand b) NH —Cl —H —Br Z484 (a and b) NH —Cl —H —F Z485 (a and b) NH —Cl—H —CF₃ Z486 (a and b) NH —Cl —H —OCH₃ Z487 (a and b) NH —Cl —H —OCH₂CH₃Z488 (a and b) NH —Cl —H —OCF₃ Z489 (a and b) NH —Cl —H -tert-butyl Z490(a and b) NH —Cl —H -iso-propyl Z491 (a and b) NH —Cl —H —OCF₃ Z492 (aand b) NH —Cl —H -tert-butyl Z493 (a and b) NH —Cl —H -iso-propyl Z494(a and b) NH —CH₃ —Cl —H Z495 (a and b) NH —CH₃ —Br —H Z496 (a and b) NH—CH₃ —F —H Z497 (a and b) NH —CH₃ —CH₃ —H Z498 (a and b) NH —CH₃ —CF₃ —HZ499 (a and b) NH —CH₃ —OCH₃ —H Z500 (a and b) NH —CH₃ —OCH₂CH₃ —H Z501(a and b) NH —CH₃ —OCF₃ —H Z502 (a and b) NH —CH₃ -tert-butyl —H Z503 (aand b) NH —CH₃ -iso-propyl —H Z504 (a and b) NH —CH₃ —CH₃ —CH₃ Z505 (aand b) NH —CH₃ —H —H Z506 (a and b) NH —CH₃ —H —Cl Z507 (a and b) NH—CH₃ —H —Br Z508 (a and b) NH —CH₃ —H —F Z509 (a and b) NH —CH₃ —H —CH₃Z510 (a and b) NH —CH₃ —H —CF₃ Z511 (a and b) NH —CH₃ —H —OCH₃ Z512 (aand b) NH —CH₃ —H —OCH₂CH₃ Z513 (a and b) NH —CH₃ —H —OCF₃ Z514 (a andb) NH —CH₃ —H -tert-butyl Z515 (a and b) NH —CH₃ —H -iso-propyl Z516 (aand b) NH —CF₃ —Cl —H Z517 (a and b) NH —CF₃ —Br —H Z518 (a and b) NH—CF₃ —F —H Z519 (a and b) NH —CF₃ —CH₃ —H Z520 (a and b) NH —CF₃ —CF₃ —HZ521 (a and b) NH —CF₃ —OCH₃ —H Z522 (a and b) NH —CF₃ —OCH₂CH₃ —H Z523(a and b) NH —CF₃ —OCF₃ —H Z524 (a and b) NH —CF₃ -tert-butyl —H Z525 (aand b) NH —CF₃ -iso-propyl —H Z526 (a and b) NH —CF₃ —CH₃ —CH₃ Z527 (aand b) NH —CF₃ —H —H Z528 (a and b) NH —CF₃ —H —Cl Z529 (a and b) NH—CF₃ —H —Br Z530 (a and b) NH —CF₃ —H —F Z531 (a and b) NH —CF₃ —H —CH₃Z532 (a and b) NH —CF₃ —H —CF₃ Z533 (a and b) NH —CF₃ —H —OCH₃ Z534 (aand b) NH —CF₃ —H —OCH₂CH₃ Z535 (a and b) NH —CF₃ —H —OCF₃ Z536 (a andb) NH —CF₃ —H -tert-butyl Z537 (a and b) NH —CF₃ —H -iso-propyl Z538 (aand b) NH —CHF₂ —Cl —H Z539 (a and b) NH —CHF₂ —Br —H Z540 (a and b) NH—CHF₂ —F —H Z541 (a and b) NH —CHF₂ —CH₃ —H Z542 (a and b) NH —CHF₂ —CF₃—H Z543 (a and b) NH —CHF₂ —OCH₃ —H Z544 (a and b) NH —CHF₂ —OCH₂CH₃ —HZ545 (a and b) NH —CHF₂ —OCF₃ —H Z546 (a and b) NH —CHF₂ -tert-butyl —HZ547 (a and b) NH —CHF₂ -iso-propyl —H Z548 (a and b) NH —CHF₂ —CH₃ —CH₃Z549 (a and b) NH —CHF₂ —H —H Z550 (a and b) NH —CHF₂ —H —Cl Z551 (a andb) NH —CHF₂ —H —Br Z552 (a and b) NH —CHF₂ —H —F Z553 (a and b) NH —CHF₂—H —CH₃ Z554 (a and b) NH —CHF₂ —H —CF₃ Z555 (a and b) NH —CHF₂ —H —OCH₃Z556 (a and b) NH —CHF₂ —H —OCH₂CH₃ Z557 (a and b) NH —CHF₂ —H —OCF₃Z558 (a and b) NH —CHF₂ —H -tert-butyl Z559 (a and b) NH —CHF₂ —H-iso-propyl Z560 (a and b) NH —OH —Cl —H Z561 (a and b) NH —OH —Br —HZ562 (a and b) NH —OH —F —H Z563 (a and b) NH —OH —CH₃ —H Z564 (a and b)NH —OH —CF₃ —H Z565 (a and b) NH —OH —OCH₃ —H Z566 (a and b) NH —OH—OCH₂CH₃ —H Z567 (a and b) NH —OH —OCF₃ —H Z568 (a and b) NH —OH-tert-butyl —H Z569 (a and b) NH —OH -iso-propyl —H Z570 (a and b) NH—OH —CH₃ —CH₃ Z571 (a and b) NH —OH —H —H Z572 (a and b) NH —OH —H —ClZ573 (a and b) NH —OH —H —Br Z574 (a and b) NH —OH —H —F Z575 (a and b)NH —OH —H —CH₃ Z576 (a and b) NH —OH —H —CF₃ Z577 (a and b) NH —OH —H—OCH₃ Z578 (a and b) NH —OH —H —OCH₂CH₃ Z579 (a and b) NH —OH —H —OCF₃Z580 (a and b) NH —OH —H -tert-butyl Z581 (a and b) NH —OH —H-iso-propyl Z582 (a and b) NH —NO₂ —Cl —H Z583 (a and b) NH —NO₂ —Br —HZ584 (a and b) NH —NO₂ —F —H Z585 (a and b) NH —NO₂ —CH₃ —H Z586 (a andb) NH —NO₂ —CF₃ —H Z587 (a and b) NH —NO₂ —OCH₃ —H Z588 (a and b) NH—NO₂ —OCH₂CH₃ —H Z589 (a and b) NH —NO₂ —OCF₃ —H Z590 (a and b) NH —NO₂-tert-butyl —H Z591 (a and b) NH —NO₂ -iso-propyl —H Z592 (a and b) NH—NO₂ —CH₃ —CH₃ Z593 (a and b) NH —NO₂ —H —H Z594 (a and b) NH —NO₂ —H—Cl Z595 (a and b) NH —NO₂ —H —Br Z596 (a and b) NH —NO₂ —H —F Z597 (aand b) NH —NO₂ —H —CH₃ Z598 (a and b) NH —NO₂ —H —CF₃ Z599 (a and b) NH—NO₂ —H —OCH₃ Z600 (a and b) NH —NO₂ —H —OCH₂CH₃ Z601 (a and b) NH —NO₂—H —OCF₃ Z602 (a and b) NH —NO₂ —H -tert-butyl Z603 (a and b) NH —NO₂ —H-iso-propyl Z604 (a and b) NH —CN —Br —H Z605 (a and b) NH —CN —Cl —HZ606 (a and b) NH —CN —F —H Z607 (a and b) NH —CN —CH₃ —H Z608 (a and b)NH —CN —CF₃ —H Z609 (a and b) NH —CN —OCH₃ —H Z610 (a and b) NH —CN—OCH₂CH₃ —H Z611 (a and b) NH —CN —OCF₃ —H Z612 (a and b) NH —CN-tert-butyl —H Z613 (a and b) NH —CN -iso-propyl —H Z614 (a and b) NH—CN —CH₃ —CH₃ Z615 (a and b) NH —CN —H —H Z616 (a and b) NH —CN —H —ClZ617 (a and b) NH —CN —H —Br Z618 (a and b) NH —CN —H —F Z619 (a and b)NH —CN —H —CH₃ Z620 (a and b) NH —CN —H —CF₃ Z621 (a and b) NH —CN —H—OCH₃ Z622 (a and b) NH —CN —H —OCH₂CH₃ Z623 (a and b) NH —CN —H —OCF₃Z624 (a and b) NH —CN —H -tert-butyl Z625 (a and b) NH —CN —H-iso-propyl Z626 (a and b) NH —Br —Br —H Z627 (a and b) NH —Br —Cl —HZ628 (a and b) NH —Br —F —H Z629 (a and b) NH —Br —CH₃ —H Z630 (a and b)NH —Br —CF₃ —H Z631 (a and b) NH —Br —OCH₃ —H Z632 (a and b) NH —Br—OCH₂CH₃ —H Z633 (a and b) NH —Br —OCF₃ —H Z634 (a and b) NH —Br-tert-butyl —H Z635 (a and b) NH —Br -iso-propyl —H Z636 (a and b) NH—Br —CH₃ —CH₃ Z637 (a and b) NH —Br —H —H Z638 (a and b) NH —Br —H —ClZ639 (a and b) NH —Br —H —Br Z640 (a and b) NH —Br —H —F Z641 (a and b)NH —Br —H —CH₃ Z642 (a and b) NH —Br —H —CF₃ Z643 (a and b) NH —Br —H—OCH₃ Z644 (a and b) NH —Br —H —OCH₂CH₃ Z645 (a and b) NH —Br —H —OCF₃Z646 (a and b) NH —Br —H -tert-butyl Z647 (a and b) NH —Br —H-iso-propyl Z648 (a and b) NH —I —Cl —H Z649 (a and b) NH —I —Br —H Z650(a and b) NH —I —F —H Z651 (a and b) NH —I —CH₃ —H Z652 (a and b) NH —I—CF₃ —H Z653 (a and b) NH —I —OCH₃ —H Z654 (a and b) NH —I —OCH₂CH₃ —HZ655 (a and b) NH —I —OCF₃ —H Z656 (a and b) NH —I -tert-butyl —H Z657(a and b) NH —I -iso-propyl —H Z658 (a and b) NH —I —CH₃ —CH₃ Z659 (aand b) NH —I —H —H Z660 (a and b) NH —I —H —Cl Z661 (a and b) NH —I —H—Br Z662 (a and b) NH —I —H —F Z663 (a and b) NH —I —H —CH₃ Z664 (a andb) NH —I —H —CF₃ Z665 (a and b) NH —I —H —OCH₃ Z666 (a and b) NH —I —H—OCH₂CH₃ Z667 (a and b) NH —I —H —OCF₃ Z668 (a and b) NH —I —H-tert-butyl Z669 (a and b) NH —I —H -iso-propyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

TABLE 27 (Iaa)

and pharmaceutically acceptable salts thereof, wherein: Compound R₁R_(8a) AA1 (a and b) —H —H AA2 (a and b) —H -tert-butyl AA3 (a and b) —H-iso-butyl AA4 (a and b) —H -sec-butyl AA5 (a and b) —H -iso-propyl AA6(a and b) —H -n-propyl AA7 (a and b) —H -cyclohexyl AA8 (a and b) —H-tert-butoxy AA9 (a and b) —H -isopropoxy AA10 (a and b) —H —CF₃ AA11 (aand b) —H —CH₂CF₃ AA12 (a and b) —H —OCF₃ AA13 (a and b) —H —Cl AA14 (aand b) —H —Br AA15 (a and b) —H —I AA16 (a and b) —H -n-butyl AA17 (aand b) —H —CH₃ AA18 (a and b) —H —SCF₃ AA19 (a and b) —H —N(CH₂CH₃)₂AA20 (a and b) —H —OCF₂CHF₂ AA21 (a and b) —H —C(OH)(CF₃)₂ AA22 (a andb) —H -(1,1-dimethyl-pentyl) AA23 (a and b) —H -(1,1-dimethyl-aceticacid) ethyl ester AA24 (a and b) —H —N-piperidinyl AA25 (a and b) —Cl —HAA26 (a and b) —Cl -tert-butyl AA27 (a and b) —Cl -iso-butyl AA28 (a andb) —Cl -sec-butyl AA29 (a and b) —Cl -iso-propyl AA30 (a and b) —Cl-n-propyl AA31 (a and b) —Cl -cyclohexyl AA32 (a and b) —Cl -tert-butoxyAA33 (a and b) —Cl -isopropoxy AA34 (a and b) —Cl —CF₃ AA35 (a and b)—Cl —CH₂CF₃ AA36 (a and b) —Cl —OCF₃ AA37 (a and b) —Cl —Cl AA38 (a andb) —Cl —Br AA39 (a and b) —Cl —I AA40 (a and b) —Cl -n-butyl AA41 (a andb) —Cl —CH₃ AA42 (a and b) —Cl —SCF₃ AA43 (a and b) —Cl —N(CH₂CH₃)₂ AA44(a and b) —Cl —OCF₂CHF₂ AA45 (a and b) —Cl —C(OH)(CF₃)₂ AA46 (a and b)—Cl -(1,1-dimethyl-pentyl) AA47 (a and b) —Cl -(1,1-dimethyl-aceticacid) ethyl ester AA48 (a and b) —Cl —N-piperidinyl AA49 (a and b) —F —HAA50 (a and b) —F -tert-butyl AA51 (a and b) —F -iso-butyl AA52 (a andb) —F -sec-butyl AA53 (a and b) —F -iso-propyl AA54 (a and b) —F-n-propyl AA55 (a and b) —F -cyclohexyl AA56 (a and b) —F -tert-butoxyAA57 (a and b) —F -isopropoxy AA58 (a and b) —F —CF₃ AA59 (a and b) —F—CH₂CF₃ AA60 (a and b) —F —OCF₃ AA61 (a and b) —F —Cl AA62 (a and b) —F—Br AA63 (a and b) —F —I AA64 (a and b) —F -n-butyl AA65 (a and b) —F—CH₃ AA66 (a and b) —F —SCF₃ AA67 (a and b) —F —N(CH₂CH₃)₂ AA68 (a andb) —F —OCF₂CHF₂ AA69 (a and b) —F —C(OH)(CF₃)₂ AA70 (a and b) —F-(1,1-dimethyl-pentyl) AA71 (a and b) —F -(1,1-dimethyl-acetic acid)ethyl ester AA72 (a and b) —F —N-piperidinyl AA73 (a and b) —CH₃ —H AA74(a and b) —CH₃ -iso-butyl AA75 (a and b) —CH₃ -tert-butyl AA76 (a and b)—CH₃ -sec-butyl AA77 (a and b) —CH₃ -iso-propyl AA78 (a and b) —CH₃-n-propyl AA79 (a and b) —CH₃ -cyclohexyl AA80 (a and b) —CH₃-tert-butoxy AA81 (a and b) —CH₃ -isopropoxy AA82 (a and b) —CH₃ —CF₃AA83 (a and b) —CH₃ —CH₂CF₃ AA84 (a and b) —CH₃ —OCF₃ AA85 (a and b)—CH₃ —Cl AA86 (a and b) —CH₃ —Br AA87 (a and b) —CH₃ —I AA88 (a and b)—CH₃ -n-butyl AA89 (a and b) —CH₃ —CH₃ AA90 (a and b) —CH₃ —SCF₃ AA91 (aand b) —CH₃ —N(CH₂CH₃)₂ AA92 (a and b) —CH₃ —OCF₂CHF₂ AA93 (a and b)—CH₃ —C(OH)(CF₃)₂ AA94 (a and b) —CH₃ -(1,1-dimethyl-pentyl) AA95 (a andb) —CH₃ -(1,1-dimethyl-acetic acid) ethyl ester AA96 (a and b) —CH₃—N-piperidinyl AA97 (a and b) —CF₃ —H AA98 (a and b) —CF₃ -tert-butylAA99 (a and b) —CF₃ -iso-butyl AA100 (a and b) —CF₃ -sec-butyl AA101 (aand b) —CF₃ -iso-propyl AA102 (a and b) —CF₃ -n-propyl AA103 (a and b)—CF₃ -cyclohexyl AA104 (a and b) —CF₃ -tert-butoxy AA105 (a and b) —CF₃-isopropoxy AA106 (a and b) —CF₃ —CF₃ AA107 (a and b) —CF₃ —CH₂CF₃ AA108(a and b) —CF₃ —OCF₃ AA109 (a and b) —CF₃ —Cl AA110 (a and b) —CF₃ —BrAA111 (a and b) —CF₃ —I AA112 (a and b) —CF₃ -n-butyl AA113 (a and b)—CF₃ —CH₃ AA114 (a and b) —CF₃ —SCF₃ AA115 (a and b) —CF₃ —N(CH₂CH₃)₂AA116 (a and b) —CF₃ —OCF₂CHF₂ AA117 (a and b) —CF₃ —C(OH)(CF₃)₂ AA118(a and b) —CF₃ -(1,1-dimethyl-pentyl) AA119 (a and b) —CF₃-(1,1-dimethyl-acetic acid) ethyl ester AA120 (a and b) —CF₃—N-piperidinyl AA121 (a and b) —CHF₂ -tert-butyl AA122 (a and b) —CHF₂—H AA123 (a and b) —CHF₂ -iso-butyl AA124 (a and b) —CHF₂ -sec-butylAA125 (a and b) —CHF₂ -iso-propyl AA126 (a and b) —CHF₂ -n-propyl AA127(a and b) —CHF₂ -cyclohexyl AA128 (a and b) —CHF₂ -tert-butoxy AA129 (aand b) —CHF₂ -isopropoxy AA130 (a and b) —CHF₂ —CF₃ AA131 (a and b)—CHF₂ —CH₂CF₃ AA132 (a and b) —CHF₂ —OCF₃ AA133 (a and b) —CHF₂ —ClAA134 (a and b) —CHF₂ —Br AA135 (a and b) —CHF₂ —I AA136 (a and b) —CHF₂-n-butyl AA137 (a and b) —CHF₂ —CH₃ AA138 (a and b) —CHF₂ —SCF₃ AA139 (aand b) —CHF₂ —N(CH₂CH₃)₂ AA140 (a and b) —CHF₂ —OCF₂CHF₂ AA141 (a and b)—CHF₂ —C(OH)(CF₃)₂ AA142 (a and b) —CHF₂ -(1,1-dimethyl-pentyl) AA143 (aand b) —CHF₂ -(1,1-dimethyl-acetic acid) ethyl ester AA144 (a and b)—CHF₂ —N-piperidinyl AA145 (a and b) —OH —H AA146 (a and b) —OH-tert-butyl AA147 (a and b) —OH -iso-butyl AA148 (a and b) —OH-sec-butyl AA149 (a and b) —OH -iso-propyl AA150 (a and b) —OH -n-propylAA151 (a and b) —OH -cyclohexyl AA152 (a and b) —OH -tert-butoxy AA153(a and b) —OH -isopropoxy AA154 (a and b) —OH —CF₃ AA155 (a and b) —OH—CH₂CF₃ AA156 (a and b) —OH —OCF₃ AA157 (a and b) —OH —Cl AA158 (a andb) —OH —Br AA159 (a and b) —OH —I AA160 (a and b) —OH -n-butyl AA161 (aand b) —OH —CH₃ AA162 (a and b) —OH —SCF₃ AA163 (a and b) —OH—N(CH₂CH₃)₂ AA164 (a and b) —OH —OCF₂CHF₂ AA165 (a and b) —OH—C(OH)(CF₃)₂ AA166 (a and b) —OH -(1,1-dimethyl-pentyl) AA167 (a and b)—OH -(1,1-dimethyl-acetic acid) ethyl ester AA168 (a and b) —OH—N-piperidinyl AA169 (a and b) —NO₂ —H AA170 (a and b) —NO₂ -tert-butylAA171 (a and b) —NO₂ -iso-butyl AA172 (a and b) —NO₂ -sec-butyl AA173 (aand b) —NO₂ -iso-propyl AA174 (a and b) —NO₂ -n-propyl AA175 (a and b)—NO₂ -cyclohexyl AA176 (a and b) —NO₂ -tert-butoxy AA177 (a and b) —NO₂-isopropoxy AA178 (a and b) —NO₂ —CF₃ AA179 (a and b) —NO₂ —CH₂CF₃ AA180(a and b) —NO₂ —OCF₃ AA181 (a and b) —NO₂ —Cl AA182 (a and b) —NO₂ —BrAA183 (a and b) —NO₂ —I AA184 (a and b) —NO₂ -n-butyl AA185 (a and b)—NO₂ —CH₃ AA186 (a and b) —NO₂ —SCF₃ AA187 (a and b) —NO₂ —N(CH₂CH₃)₂AA188 (a and b) —NO₂ —OCF₂CHF₂ AA189 (a and b) —NO₂ —C(OH)(CF₃)₂ AA190(a and b) —NO₂ -(1,1-dimethyl-pentyl) AA191 (a and b) —NO₂-(1,1-dimethyl-acetic acid) ethyl ester AA192 (a and b) —NO₂—N-piperidinyl AA193 (a and b) —CN —H AA194 (a and b) —CN -tert-butylAA195 (a and b) —CN -iso-butyl AA196 (a and b) —CN -sec-butyl AA197 (aand b) —CN -iso-propyl AA198 (a and b) —CN -n-propyl AA199 (a and b) —CN-cyclohexyl AA200 (a and b) —CN -tert-butoxy AA201 (a and b) —CN-isopropoxy AA202 (a and b) —CN —CF₃ AA203 (a and b) —CN —CH₂CF₃ AA204(a and b) —CN —OCF₃ AA205 (a and b) —CN —Cl AA206 (a and b) —CN —BrAA207 (a and b) —CN —I AA208 (a and b) —CN -n-butyl AA209 (a and b) —CN—CH₃ AA210 (a and b) —CN —SCF₃ AA211 (a and b) —CN —N(CH₂CH₃)₂ AA212 (aand b) —CN —OCF₂CHF₂ AA213 (a and b) —CN —C(OH)(CF₃)₂ AA214 (a and b)—CN -(1,1-dimethyl-pentyl) AA215 (a and b) —CN -(1,1-dimethyl-aceticacid) ethyl ester AA216 (a and b) —CN —N-piperidinyl AA217 (a and b) —Br—H AA218 (a and b) —Br -tert-butyl AA219 (a and b) —Br -iso-butyl AA220(a and b) —Br -sec-butyl AA221 (a and b) —Br -iso-propyl AA222 (a and b)—Br -n-propyl AA223 (a and b) —Br -cyclohexyl AA224 (a and b) —Br-tert-butoxy AA225 (a and b) —Br -isopropoxy AA226 (a and b) —Br —CF₃AA227 (a and b) —Br —CH₂CF₃ AA228 (a and b) —Br —OCF₃ AA229 (a and b)—Br —Cl AA230 (a and b) —Br —Br AA231 (a and b) —Br —I AA232 (a and b)—Br -n-butyl AA233 (a and b) —Br —CH₃ AA234 (a and b) —Br —SCF₃ AA235 (aand b) —Br —N(CH₂CH₃)₂ AA236 (a and b) —Br —OCF₂CHF₂ AA237 (a and b) —Br—C(OH)(CF₃)₂ AA238 (a and b) —Br -(1,1-dimethyl-pentyl) AA239 (a and b)—Br -(1,1-dimethyl-acetic acid) ethyl ester AA240 (a and b) —Br—N-piperidinyl AA241 (a and b) —I -tert-butyl AA242 (a and b) —I —HAA243 (a and b) —I -iso-butyl AA244 (a and b) —I -sec-butyl AA245 (a andb) —I -iso-propyl AA246 (a and b) —I -n-propyl AA247 (a and b) —I-cyclohexyl AA248 (a and b) —I -tert-butoxy AA249 (a and b) —I-isopropoxy AA250 (a and b) —I —CF₃ AA251 (a and b) —I —CH₂CF₃ AA252 (aand b) —I —OCF₃ AA253 (a and b) —I —Cl AA254 (a and b) —I —Br AA255 (aand b) —I —I AA256 (a and b) —I -n-butyl AA257 (a and b) —I —CH₃ AA258(a and b) —I —SCF₃ AA259 (a and b) —I —N(CH₂CH₃)₂ AA260 (a and b) —I—OCF₂CHF₂ AA261 (a and b) —I —C(OH)(CF₃)₂ AA262 (a and b) —I-(1,1-dimethyl-pentyl) AA263 (a and b) —I -(1,1-dimethyl-acetic acid)ethyl ester AA264 (a and b) —I —N-piperidinyl (a) means that R₃ is —H.(b) means that R₃ is —CH₃.

4.2 Definitions

As used in connection with the Cyclo(hetero)alkenyl Compounds herein,the terms used above having following meaning:

“—(C₁-C₁₀)alkyl” means a straight chain or branched non-cyclichydrocarbon having from 1 to 10 carbon atoms. Representative straightchain —(C₁-C₁₀)alkyls include -methyl, -ethyl, -n-propyl, -n-butyl,-n-pentyl, -n-hexyl, -n-heptyl, -n-octyl, -n-nonyl, and -n-decyl.Representative branched —(C₁-C₁₀)alkyls include -iso-propyl, -sec-butyl,-iso-butyl, -tert-butyl, -iso-pentyl, -neopentyl, 1-methylbutyl,2-methylbutyl, 3-methylbutyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl,1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl,1-ethylbutyl, 2-ethylbutyl, 3-ethylbutyl, 1,1-dimethylbutyl,1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl,2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-methylhexyl, 2-methylhexyl,3-methylhexyl, 4-methylhexyl, 5-methylhexyl, 1,2-dimethylpentyl,1,3-dimethylpentyl, 1,2-dimethylhexyl, 1,3-dimethylhexyl,3,3-dimethylhexyl, 1,2-dimethylheptyl, 1,3-dimethylheptyl, and3,3-dimethylheptyl.

“—(C₁-C₆)alkyl” means a straight chain or branched non-cyclichydrocarbon having from 1 to 6 carbon atoms. Representative straightchain —(C₁-C₆)alkyls include -methyl, -ethyl, -n-propyl, -n-butyl,-n-pentyl, and -n-hexyl. Representative branched —(C₁-C₆)alkyls include-iso-propyl, -sec-butyl, -iso-butyl, -tert-butyl, -iso-pentyl,-neopentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl,1,1-dimethylpropyl, 1,2-dimethylpropyl, 1-methylpentyl, 2-methylpentyl,3-methylpentyl, 4-methylpentyl, 1-ethylbutyl, 2-ethylbutyl,3-ethylbutyl, 1,1-dimethtylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl,2,2-dimethylbutyl, 2,3-dimethylbutyl, and 3,3-dimethylbutyl.

“—(C₁-C₄)alkyl” means a straight chain or branched non-cyclichydrocarbon having from 1 to 4 carbon atoms. Representative straightchain —(C₁-C₄)alkyls include -methyl, -ethyl, -n-propyl, and -n-butyl.Representative branched —(C₁-C₄)alkyls include -iso-propyl, -sec-butyl,-iso-butyl, and -tert-butyl.

“—(C₂-C₁₀)alkenyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 10 carbon atoms and including at least onecarbon-carbon double bond. Representative straight chain and branched(C₂-C₁₀)alkenyls include -vinyl, -allyl, -1-butenyl, -2-butenyl,-iso-butylenyl, -1-pentenyl, -2-pentenyl, -3-methyl-1-butenyl,-2-methyl-2-butenyl, -2,3-dimethyl-2-butenyl, -1-hexenyl, -2-hexenyl,-3-hexenyl, -1-heptenyl, -2-heptenyl, -3-heptenyl, -1-octenyl,-2-octenyl, -3-octenyl, -1-nonenyl, -2-nonenyl, -3-nonenyl, -1-decenyl,-2-decenyl, -3-decenyl and the like.

“—(C₂-C₆)alkenyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 6 carbon atoms and including at least onecarbon-carbon double bond. Representative straight chain and branched(C₂-C₆)alkenyls include -vinyl, -allyl, -1-butenyl, -2-butenyl,-iso-butylenyl, -1-pentenyl, -2-pentenyl, -3-methyl-1-butenyl,-2-methyl-2-butenyl, -2,3-dimethyl-2-butenyl, -1-hexenyl, 2-hexenyl,3-hexenyl and the like.

“—(C₂-C₁₀)alkynyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 10 carbon atoms and including at least onecarbon-carbon triple bond. Representative straight chain and branched—(C₂-C₁₀)alkynyls include -acetylenyl, -propynyl, -1-butynyl,-2-butynyl, -1-pentynyl, -2-pentynyl, -3-methyl-1-butynyl, -4-pentynyl,-1-hexynyl, -2-hexynyl, -5-hexynyl, -1-heptynyl, -2-heptynyl,-6-heptynyl, -1-octynyl, -2-octynyl, -7-octynyl, -1-nonynyl, -2-nonynyl,-8-nonynyl, -1-decynyl, -2-decynyl, -9-decynyl and the like.

“—(C₂-C₆)alkynyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 6 carbon atoms and including at least onecarbon-carbon triple bond. Representative straight chain and branched(C₂-C₆)alkynyls include -acetylenyl, -propynyl, -1-butynyl, -2-butynyl,-1-pentynyl, -2-pentynyl, -3-methyl-1-butynyl, -4-pentynyl, -1-hexynyl,-2-hexynyl, -5-hexynyl and the like.

“—(C₃-C₁₀)cycloalkyl” means a saturated cyclic hydrocarbon having from 3to 10 carbon atoms. Representative (C₃-C₁₀)cycloalkyls are -cyclopropyl,-cyclobutyl, -cyclopentyl, -cyclohexyl, -cycloheptyl, -cyclooctyl,-cyclononyl, and -cyclodecyl.

“—(C₃-C₈)cycloalkyl” means a saturated cyclic hydrocarbon having from 3to 8 carbon atoms. Representative (C₃-C₈)cycloalkyls include-cyclopropyl, -cyclobutyl, -cyclopentyl, -cyclohexyl, -cycloheptyl, and-cyclooctyl.

“—(C₈-C₁₄)bicycloalkyl” means a bi-cyclic hydrocarbon ring system havingfrom 8 to 14 carbon atoms and at least one saturated cyclic alkyl ring.Representative —(C₈-C₁₄)bicycloalkyls include -indanyl,-1,2,3,4-tetrahydronaphthyl, -5,6,7,8-tetrahydronaphthyl,-perhydronaphthyl and the like.

“—(C₈-C₁₄)tricycloalkyl” means a tri-cyclic hydrocarbon ring systemhaving from 8 to 14 carbon atoms and at least one saturated cyclic alkylring. Representative —(C₈-C₁₄)tricycloalkyls include -pyrenyl,-1,2,3,4-tetrahydroanthracenyl, -perhydroanthracenyl -aceanthreneyl,-1,2,3,4-tetrahydropenanthrenyl, -5,6,7,8-tetrahydrophenanthrenyl,-perhydrophenanthrenyl and the like.

“—(C₅-C₁₀)cycloalkenyl” means a cyclic non-aromatic hydrocarbon havingat least one carbon-carbon double bond in the cyclic system and from 5to 10 carbon atoms. Representative (C₅-C₁₀)cycloalkenyls include-cyclopentenyl, -cyclopentadienyl, -cyclohexenyl, -cyclohexadienyl,-cycloheptenyl, -cycloheptadienyl, -cycloheptatrienyl, -cyclooctenyl,-cyclooctadienyl, -cyclooctatrienyl, -cyclooctatetraenyl, -cyclononenyl,-cyclononadienyl, -cyclodecenyl, -cyclodecadienyl and the like.

“—(C₅-C₈)cycloalkenyl” means a cyclic non-aromatic hydrocarbon having atleast one carbon-carbon double bond in the cyclic system and from 5 to 8carbon atoms. Representative (C₅-C₈)cycloalkenyls include-cyclopentenyl, -cyclopentadienyl, -cyclohexenyl, -cyclohexadienyl,-cycloheptenyl, -cycloheptadienyl, -cycloheptatrienyl, -cyclooctenyl,-cyclooctadienyl, -cyclooctatrienyl, -cyclooctatetraenyl and the like.

“—(C₈-C₁₄)bicycloalkenyl” means a bi-cyclic hydrocarbon ring systemhaving at least one carbon-carbon double bond in each ring and from 8 to14 carbon atoms. Representative —(C8-C14)bicycloalkenyls include-indenyl, -pentalenyl, -naphthalenyl, -azulenyl, -heptalenyl,-1,2,7,8-tetrahydronaphthalenyl and the like.

“—(C₈-C₁₄)tricycloalkenyl” means a tri-cyclic hydrocarbon ring systemhaving at least one carbon-carbon double bond in each ring and from 8 to14 carbon atoms. Representative —(C₈-C₁₄)tricycloalkenyls include-anthracenyl, -phenanthrenyl, -phenalenyl, -acenaphthalenyl,as-indacenyl, s-indacenyl and the like.

“-(3- to 7-membered)heterocycle” or “-(3- to 7-membered)heterocyclo”means a 3- to 7-membered monocyclic heterocyclic ring which is eithersaturated, unsaturated non-aromatic, or aromatic. A 3- or a 4-memberedheterocycle can contain up to 3 heteroatoms, a 5-membered heterocyclecan contain up to 4 heteroatoms, a 6-membered heterocycle can contain upto 6 heteroatoms, and a 7-membered heterocycle can contain up to 7heteroatoms. Each heteroatom is independently selected from nitrogen,which can be quaternized; oxygen; and sulfur, including sulfoxide andsulfone. The -(3- to 7-membered)heterocycle can be attached via anitrogen or carbon atom. Representative -(3- to 7-membered)heterocyclesinclude pyridyl, furyl, thiophenyl, pyrrolyl, oxazolyl, imidazolyl,thiazolyl, thiadiazolyl, isoxazolyl, pyrazolyl, isothiazolyl,pyridazinyl, pyrimidinyl, pyrimidinyl, triazinyl, morpholinyl,pyrrolidinonyl, pyrrolidinyl, piperidinyl, piperazinyl, hydantoinyl,valerolactamyl, oxiranyl, oxetanyl, tetrahydrofuranyl,tetrahydropyranyl, tetrahydropyrindinyl, tetrahydropyrimidinyl,tetrahydrothiophenyl, tetrahydrothiopyranyl and the like.

“-(3- to 5-membered)heterocycle” or “-(3- to 5-membered)heterocyclo”means a 3- to 5-membered monocyclic heterocyclic ring which is eithersaturated, unsaturated non-aromatic, or aromatic. A 3- or 4-memberedheterocycle can contain up to 3 heteroatoms and a 5-membered heterocyclecan contain up to 4 heteroatoms. Each heteroatom is independentlyselected from nitrogen, which can be quaternized; oxygen; and sulfur,including sulfoxide and sulfone. The -(3- to 5-membered)heterocycle canbe attached via a nitrogen or carbon atom. Representative -(3- to5-membered)heterocycles include furyl, thiophenyl, pyrrolyl, oxazolyl,imidazolyl, thiazolyl, isoxazolyl, pyrazolyl, isothiazolyl, triazinyl,pyrrolidinonyl, pyrrolidinyl, hydantoinyl, oxiranyl, oxetanyl,tetrahydrofuranyl, tetrahydrothiophenyl and the like.

“-(7- to 10-membered)bicycloheterocycle” or “-(7- to10-membered)bicycloheterocyclo” means a 7- to 10-membered bicyclic,heterocyclic ring which is either saturated, unsaturated non-aromatic,or aromatic. A -(7- to 10-membered)bicycloheterocycle contains from 1 to4 heteroatoms independently selected from nitrogen, which can bequaternized; oxygen; and sulfur, including sulfoxide and sulfone. The-(7- to 10-membered)bicycloheterocycle can be attached via a nitrogen orcarbon atom. Representative -(7- to 10-membered)bicycloheterocyclesinclude -quinolinyl, -isoquinolinyl, -chromonyl, -coumarinyl, -indolyl,-indolizinyl, -benzo[b]furanyl, -benzo[b]thiophenyl, -indazolyl,-purinyl, -4H-quinolizinyl, -isoquinolyl, -quinolyl, -phthalazinyl,-naphthyridinyl, -carbazolyl, -β-carbolinyl and the like.

“—(C₁₄)aryl” means a 14-membered aromatic carbocyclic moiety such as-anthryl or -phenanthryl.

“-(5- to 10-membered)heteroaryl” means an aromatic heterocycle ring of 5to 10 members, including both mono- and bicyclic ring systems, whereinat least one carbon atom of one or both of the rings is replaced with aheteroatom independently selected from nitrogen, oxygen, and sulfur. Inone embodiment one of the -(5- to 10-membered)heteroaryl's rings containat least one carbon atom. In another embodiment both of the -(5- to10-membered)heteroaryl's rings contain at least one carbon atom.Representative -(5- to 10-membered)heteroaryls include pyridyl, furyl,benzofuranyl, thiophenyl, benzothiophenyl, quinolinyl, pyrrolyl,indolyl, oxazolyl, benzoxazolyl, imidazolyl, benzimidazolyl, thiazolyl,benzothiazolyl, isoxazolyl, pyrazolyl, isothiazolyl, pyridazinyl,pyrimidinyl, pyrimidinyl, thiadiazolyl, triazinyl, cinnolinyl,phthalazinyl, and quinazolinyl.

“—CH₂(halo)” means a methyl group wherein one of the hydrogens of themethyl group has been replaced with a halogen. Representative —CH₂(halo)groups include —CH₂F, —CH₂Cl, —CH₂Br, and —CH₂I.

“—CH(halo)₂” means a methyl group wherein two of the hydrogens of themethyl group have been replaced with a halogen. Representative—CH(halo)₂ groups include —CHF₂, —CHCl₂, —CHBr₂, —CHBrCl, —CHClI, and—CHI₂.

“—C(halo)₃” means a methyl group wherein each of the hydrogens of themethyl group has been replaced with a halogen. Representative —C(halo)₃groups include —CF₃, —CCl₃, —CBr₃, and —CI₃.

“-Halogen” or “-Halo” means —F, —Cl, —Br, or —I.

The phrase “pyridyl group” means

wherein R₁, R₂, and n are defined above for the Cyclo(hetero)alkenylCompounds of Formula (I).

The phrase “pyrazinyl group” means,

wherein R₁, R₂, and p are defined above for the Cyclo(hetero)alkenylCompounds of Formula (I).

The phrase “pyrimidinyl group” means

wherein R₁, R₂, and p are defined above for the Cyclo(hetero)alkenylCompounds of Formula (I).

The phrase “pyridazinyl group” means

wherein R₁, R₂, and p are defined above for the Cyclo(hetero)alkenylCompounds of Formula (I).

The phrase “thiadiazolyl group” means

wherein R₁ is defined above for the Cyclo(hetero)alkenyl Compounds ofFormula (I).

The phrase “benzoimidazolyl group” means

wherein R₈ and s are defined above for the Cyclo(hetero)alkenylCompounds of Formula (I).

The phrase “benzothiazolyl group” means

wherein R₈ and s are defined above for the Cyclo(hetero)alkenylCompounds of Formula (I).

The phrase “benzooxazolyl group” means

wherein R₈ and s are defined above for the Cyclo(hetero)alkenylCompounds of Formula (I).

The phrase “5-benzodioxolyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-benzodithiolyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-dihydroindenyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-dihydrobenzoimidazolyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “6-dihydrobenzofuranyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-dihydrobenzofuranyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “6-indolinyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-indolinyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “6-dihydrobenzothiopheneyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-dihydrobenzothiopheneyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-dihydrobenzooxazolyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “6-dihydrobenzooxazolyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “5-dihydrobenzothiazolyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “6-dihydrobenzothiazolyl group” means

where each R₉ is independently —H, -halo, or —(C₁-C₆)alkyl.

The phrase “2-(3-chloropyridyl)” means

The phrase “2-(3-fluoropyridyl)” means

The phrase “2-(3-methylpyridyl)” means

The phrase “2-(3-CF₃-pyridyl)” means

The phrase “2-(3-CHF₂-pyridyl)” means

The phrase “2-(3-hydroxypyridyl)” means

The phrase “2-(3-nitropyridyl)” means

The phrase “2-(3-cyanopyridyl)” means

The phrase “2-(3-bromopyridyl)” means

The phrase “2-(3-iodopyridyl)” means

The phrase “4-(5-chloropyrimidinyl)” means

The phrase “3-(4-chloropyridazinyl)” means

The phrase “3-(4-methylpyridazinyl)” means

The phrase “3-(4-fluoropyridazinyl)” means

The phrase “5-(4-chlorothiadiazolyl)” means

The phrase “5-(4-methylthiadiazolyl)” means

The phrase “4-(5-methylpyrimidinyl)” means

The phrase “4-(5-fluoropyrimidinyl)” means

The phrase “2-(3-chloropyrazinyl)” means

The phrase “2-(3-methylpyrazinyl)” means

The phrase “2-(3-fluoropyrazinyl)” means

The phrase “5-(4-fluorothiadiazolyl)” means

The phrase “-(1,1-dimethyl-pentyl)” means

The phrases “-(1,1-dimethyl-acetic acid) ethyl ester” and“2-methylpropionic acid ethyl ester” mean

The phrases “—(N-piperidinyl)” and “(piperidin-1-yl)-” mean

The phrase “cyclo(hetero)alkenyl ring” means

wherein V, R₃ and m are defined above and the numbers designate theposition of each atom of the cyclo(hetero)alkenyl ring. The language“(hetero)” means that V is either: N, in which case thecyclo(hetero)alkenyl ring is a tetrahydropyridyl ring; or CH, in whichcase the cyclo(hetero)alkenyl ring is a cycloalkenyl ring.

The term “animal,” includes, but is not limited to, a cow, monkey,baboon, chimpanzee, horse, sheep, pig, chicken, turkey, quail, cat, dog,mouse, rat, rabbit, guinea pig, and human.

The phrase “pharmaceutically acceptable salt,” as used herein, is anypharmaceutically acceptable salt that can be prepared from aCyclo(hetero)alkenyl Compound, including a salt formed from an acid anda basic functional group, such as a nitrogen group, of one of theCyclo(hetero)alkenyl Compounds. Illustrative salts include, but are notlimited, to sulfate, citrate, acetate, oxalate, chloride, bromide,iodide, nitrate, bisulfate, phosphate, acid phosphate, isonicotinate,lactate, salicylate, acid citrate, tartrate, oleate, tannate,pantothenate, bitartrate, ascorbate, succinate, maleate, gentisinate,fumarate, gluconate, glucoronate, saccharate, formate, benzoate,glutamate, methanesulfonate, ethanesulfonate, benzenesulfonate,p-toluenesulfonate, and pamoate (i.e.,1,1′-methylene-bis-(2-hydroxy-3-naphthoate)) salts. The term“pharmaceutically acceptable salt” also includes a salt prepared from aCyclo(hetero)alkenyl Compound having an acidic functional group, such asa carboxylic acid functional group, and a pharmaceutically acceptableinorganic or organic base. Suitable bases include, but are not limitedto, hydroxides of alkali metals such as sodium, potassium, and lithium;hydroxides of alkaline earth metal such as calcium and magnesium;hydroxides of other metals, such as aluminum and zinc; ammonia andorganic amines, such as unsubstituted or hydroxy-substituted mono-, di-,or trialkylamines; dicyclohexylamine; tributyl amine; pyridine;N-methyl, N-ethylamine; diethylamine; triethylamine; mono-, bis-, ortris-(2-hydroxy-lower alkyl amines), such as mono-, bis-, ortris-(2-hydroxyethyl)amine, 2-hydroxy-tert-butylamine, ortris-(hydroxymethyl)methylamine, N,N,-di-lower alkyl-N-(hydroxy loweralkyl)-amines, such as N,N,-dimethyl-N-(2-hydroxyethyl)amine, ortri-(2-hydroxyethyl)amine; N-methyl-D-glucamine; and amino acids such asarginine, lysine and the like.

The phrase “effective amount,” when used in connection with aCyclo(hetero)alkenyl Compound means an amount effective for: (a)treating or preventing a Condition; or (b) inhibiting VR1, mGluR1, ormGluR5 function in a cell.

The phrase “effective amount,” when used in connection with anothertherapeutic agent means an amount for providing the therapeutic effectof the other therapeutic agent.

When a first group is “substituted with one or more” second groups, oneor more hydrogen atoms of the first group is replaced with acorresponding number of second groups. When the number of second groupsis two or greater, each second group can be the same or different. Inone embodiment, the number of second groups is one or two. In anotherembodiment, the number of second groups is one.

The term “THF” means tetrahydrofuran.

The term “DCM” means dichloromethane.

The term “DCE” means dichloroethane, e.g., 1,1-dichloroethane,1,2-dichloroethane, or mixtures thereof.

The term “DMF” means dimethylformamide.

The term “DMSO” means dimethyl sulfoxide.

The term “DIEA” means diisopropylethylamine.

The term “TFA” means trifluoroacetic acid.

The term “EtOAc” means ethyl acetate.

The term “Dppp” means 1,3-bis(diphenylphosphino)propane.

The term “Pd(OAc)₂” means palladium acetate.

The term “IBD” means inflammatory-bowel disease.

The term “IBS” means irritable-bowel syndrome.

The term “ALS” means amyotrophic lateral sclerosis.

The term “LiHMDS” means lithium hexamethyldisilazide.

The phrases “treatment of,” “treating” and the like include theamelioration or cessation of a Condition or a symptom thereof.

In one embodiment, treating includes inhibiting, for example, decreasingthe overall frequency of episodes of a Condition or a symptom thereof.

The phrases “prevention of,” “preventing” and the like include theavoidance of the onset of a Condition or a symptom thereof.

4.3 Methods for Making the Cyclo(Hetero)Alkenyl Compounds

The Cyclo(hetero)alkenyl Compounds can be made using conventionalorganic synthesis or by the following illustrative methods shown in theschemes below.

4.3.1 Methods for Making the Cyclo(Hetero)Alkenyl Compounds where V is N

In one embodiment, the present invention relates to methods for makingthe Cyclo(hetero)alkenyl Compounds where V is N by the followingnon-limiting illustrative method shown below in Scheme A.

where R₁, R₂, R₃, R₄, Ar¹, Ar², m, n and p are defined above and Z_(a)is a halogen.

About 1 eq. of a Compound of Formula 1 a-h (1M) and 1 eq. of a Compoundof Formula 2 are heated in DMSO in the presence of about 1 eq. of DMA ata temperature of from about 125° C. to about 140° C. for about 12 h. Theresulting reaction mixture is cooled to about 25° C. and the solventremoved, e.g., under reduced pressure, to provide an8-heteroaromatic-1,4-dioxa-8-aza-spiro[4.5]decane Compound of Formula 3a-h. A Compound of Formula 3 a-h is useful, e.g., as an intermediate forthe synthesis of a Cyclo(hetero)alkenyl Compound.

The Compound of Formula 3 a-h can also be obtained by dissolving about 1equivalent of a Compound of Formula 1 a-h (1.5M), a Compound of Formula2 (about 1.2 eq.), and the sodium salt of 2-methylpropan-2-ol (“NaOtBu”,1.5 eq.) in glyme and degassing the resulting solution by bubblingnitrogen through the solution. After the solution is degassed,tris-(dibenzylideneacetone)dipalladium (0) catalyst (0.02 eq.) and 0.02eq. of the ligand depicted below

is added to the solution and the resulting reaction mixture is heated ata temperature of about 50° C. for about 4.5 h. The reaction mixture iscooled to about 25° C. and solids removed by filtering over CELITE. Thesolvent is then removed, e.g., under reduced pressure, to provide aresidue. The resulting residue can be purified, e.g., using a silica gelcolumn eluted with 6:1 hexane:ethyl acetate.

The Compound of Formula 3 a-h can also be obtained by by dissolving,e.g., in toluene, about 1 equivalent of a Compound of Formula 1 a-h(1.2M), adding to the solution a Compound of Formula 2 (about 1.1 eq.),followed by the addition of NaOtBu (about 1.1 eq.), Pd(OAc)₂ (about 0.05eq.), and 0.05 eq. Dppp (about 0.05 eq.) to form a reaction mixture. Theatmosphere in contact with the reaction mixture is replaced by nitrogen.The reaction mixture is stirred and heated to a temperature of fromabout 25° C. to about the boiling point of the solvent, alternately fromabout 50° C. to about 100° C., for about 3 h. The reaction mixture iscooled to about 25° C. and worked-up, e.g., as described above, toprovide the Compound of Formula 3 a-h.

The Compound of Formula 3 a-h is then reacted with an acid to provide aCompound of Formula 4 a-h. In one embodiment, the present inventionrelates to a method for making a Cyclo(hetero)alkenyl Compoundcomprising allowing a Compound of Formula 3 a-h to react with an acid.In another embodiment, the acid is an organic acid, such as TFA, aninorganic acid, such as hydrochloric acid, or their mixtures. Forexample, the Compound of Formula 3 a-h (0.25M) is reacted with 30% TFAin DCM at a temperature of from about 25° C. to about the boiling pointof the solvent. Alternatively, the Compound of Formula 3 a-h (0.25M) isreacted with about 4N HCl in THF at a temperature of about 50° C. forabout 16 hours. Either resulting reaction mixture is cooled to about 25°C. and neutralized with aqueous Na₂CO₃ such that separate aqueous andorganic layers form. The organic layer is separated from the aqueouslayer. The aqueous layer is then extracted with DCM and the organiclayer and the post-extraction DCM are combined and dried, e.g., withMgSO₄ or Na₂SO₄. The solvent is removed, e.g., under reduced pressure,to provide a 1-heteroaromatic-piperidin-4-one Compound of Formula 4 a-h.The Compound of Formula 4 a-h can be purified, e.g., using a silica gelcolumn eluted with 15:1 hexane:ethyl acetate. A Compound of Formula 4a-h is useful, e.g., as an intermediate for the synthesis of aCyclo(hetero)alkenyl Compound.

In one embodiment, the present invention relates to a method for makinga Cyclo(hetero)alkenyl Compound comprising allowing a Compound ofFormula 4 a-h to react with LiHMDS and then an excess triflimide. Forexample, the Compound of Formula 4 a-h (1 eq.) is reacted with 1.25 eq.of LiHMDS at about −78° C. and the resulting reaction mixture allowed tostir at about −78° C. for about 2 h. After stirring for about 2 h, anexcess of N-(5-chloro-2-pyridyl)triflimide 5 (1.05 eq. in oneembodiment, 3 eq. in another embodiment) is added to the reactionmixture at a temperature of about −78° C. The reaction mixture isstirred for about 2.5 h at a temperature of about −78° C. and thenallowed to warm to about 25° C. The solvent is removed, e.g., underreduced pressure, to provide a residue that can be purified, e.g., usinga silica gel column eluted with 10:1 hexane:ethyl acetate to provide aCompound of Formula 6 a-h. A Compound of Formula 6 a-h is useful, e.g.,as an intermediate for the synthesis of a Cyclo(hetero)alkenyl Compound.

In one embodiment, the present invention relates to a method for makinga Cyclo(hetero)alkenyl Compound comprising allowing a Compound ofFormula 6 a-h to react with a compound of formula Ar²—NHR₄. In anotherembodiment, the reaction in the presence of an organic base, e.g., atrialkylamine. In another embodiment, the reaction in the presence ofPd(OAc)₂ and Dppp. In another embodiment, the reaction in the presenceof a carbon monoxide atmosphere. For example, about 1 equivalent of theCompound of Formula 6 a-h (about 1M), an excess of a compound of formulaAr²—NHR₄ (about 2 eq.), and a trialkylamine, e.g., triethylamine (fromabout 1.1 to about 20 eq., about 2.2 eq. in one embodiment), aredissolved in DMF or THF and the resulting solution is degassed bybubbling nitrogen through the solution. Pd(OAc)₂ and Dppp (about 0.2-0.3eq. of each) are added to the solution and the nitrogen atmosphere isreplaced with carbon monoxide at a pressure of about 1 atm. The reactionmixture is then heated to about 70° C. for about 2 h. The reactionmixture is cooled to about 25° C. and the solvent removed, e.g., underreduced pressure, to provide a residue. The resulting residue can bepurified, e.g., using a silica gel column eluted with 10:1 hexane:ethylacetate. Where m=1, a mixture of Cyclo(hetero)alkenyl Compounds isgenerally obtained. The mixture can be separated by conventionalmethods, for example, column chromatography.

Compounds of formula 2 are commercially available or can be prepared bymethods known to those skilled in the art.

The Compound of Formula (I) where X is S (i.e., the Compound of Formula(II′)) can be made by, e.g., reacting a Compound of Formula (II) (i.e.,where X is O) with Lawesson's reagent (i.e.,2,4-bis(4-methoxyphenyl)-1,3-dithia-2,4-diphosphetane-2,4-disulfide)according to the procedures described in Chem. Let. 8:713-4 (1995) orChem. Let. 12:1398-9 (2000). In one embodiment, the Compound of Formula(I) where X is S can be made by reacting a Compound of Formula (II)(where X is O) with Lawesson's reagent in a nonpolar solvent such as THFor toluene at a temperature of about 100° C. for about 2-3 hours, asshown below:

In another embodiment, the present invention relates to methods formaking the Cyclo(hetero)alkenyl Compounds where V is N from the8-heteroaromatic-1,4-dioxa-8-aza-spiro[4.5]decane Compounds of Formula 3a-h by the following non-limiting illustrative method shown below inScheme B.

where R₃, R₄, Ar¹, Ar², and m are defined above.

In Step B1 of Scheme B, the Compound of Formula 3 a-h, which can beobtained, e.g., as described in Scheme A, is reacted with aketone-forming reagent, e.g., an inorganic acid such as HCl or H₂SO₄, oran organic acid, such as trifluoroacetic acid. In one embodiment, thepresent invention relates to a method for making a Cyclo(hetero)alkenylCompound comprising allowing a Compound of Formula 3 a-h to react with aketone-forming reagent. In another embodiment, the ketone-formingreagent is HCl, H₂SO₄, trifluoroacetic acid or a mixture thereof. Inanother embodiment, the ketone-forming reagent is HCl. In anotherembodiment, the ketone-forming reagent is H₂SO₄. In another embodiment,the ketone-forming reagent is trifluoroacetic acid.

In certain embodiments, the ketone-forming reagent is present in thereaction in Step B1 at an initial concentration within the range of fromabout 1N to about 12N, or at an initial concentration within the rangeof from about 2N to about 6N. In a specific embodiment, theketone-forming reagent is present in the reaction at an initialconcentration of about 4N.

In certain embodiments, the Compound of Formula 3 a-h is present in thereaction in Step B1 at an initial concentration within the range of fromabout 0.05M to about 10M, or at an initial concentration within therange of from about 0.1M to about 1M. In a specific embodiment, theCompound of Formula 3 a-h is present in the reaction at an initialconcentration of about 0.25M.

In certain embodiments, the reaction in Step B1 is carried out at atemperature within the range of from about 0° C. to about the boilingpoint of the solvent; at a temperature within the range of from about15° C. to about 100° C.; or at a temperature within the range of fromabout 45° C. to about 55° C.

In certain embodiments, the reaction in Step B1 is carried out in anonpolar solvent, e.g., hexane, heptane, benzene, diethyl ether, THF,pyridine, DCM, DCE, chloroform, carbon tetrachloride and combinationsthereof. In one embodiment, the nonpolar solvent is THF, chloroform orcombinations thereof. In another embodiment, the nonpolar solvent is THEIn another embodiment, the nonpolar solvent is chloroform.

In certain embodiments, the Compound of Formula 3 a-h is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with theketone-forming reagent. For example, the hydrochloride salt of theCompound of Formula 3 a-h is dissolved in a suitable organic solventsuch as but not limited to chloroform, to provide a solution that isextracted with, e.g., a saturated aqueous solution of Na₂CO₃. Theorganic layer is recovered and the aqueous layer back-extracted with anadditional volume of the organic solvent. The organic solvent layers arecombined, extracted with water, dried, e.g., over anhydrous sodiumsulfate, and then the liquid is removed, such as by evaporation underreduced pressure, e.g., with a rotary evaporator, to provide theCompound of Formula 3 a-h as the free amine.

The reaction in Step B1 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step B1 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step B1 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step B1 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step B1 is carried out under an argonatmosphere.

Progress of the reaction in Step B1 can be monitored using conventionalanalytical techniques, including but not limited to infraredspectroscopy (“IR”), liquid chromatography (“LC”), mass spectrometry(“MS”), liquid chromatography in conjunction with mass spectrometry(“LCMS”), thin-layer chromatography (“TLC”), high-performance liquidchromatography (“HPLC”), gas chromatography (“GC”), gas-liquidchromatography (“GLC”), and/or nuclear magnetic resonance spectroscopy(“NMR”), such as ¹H and ¹³C NMR. The reaction according to Step B1 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a Compound ofFormula 4 a-h, to starting material, the Compound of Formula 3 a-h,remains essentially constant. Typically, a time sufficient for thereaction in Step B1 is within the range of from about 0.5 hours to about48 hours, from about 1 hour to about 24 hours, or from about 6 hours toabout 18 hours. In a specific embodiment, the reaction according to StepB1 is carried out for about 16 hours.

In another embodiment, the reaction according to Step B1 is carried outas described in Scheme A. In another embodiment, the reaction accordingto Step B1 is carried out in THF with the Compound of Formula 3 a-hpresent at an initial concentration of about 0.35M, with about a 4Ninitial concentration of HCl, at a temperature of about 50° C., and fora period of about 16 hours with stirring.

The resulting reaction mixture is cooled to about 25° C. andneutralized, e.g., with aqueous Na₂CO₃, such that separate aqueous andorganic layers form. The organic layer is separated from the aqueouslayer. The aqueous layer is then extracted, e.g., with ethyl acetate.The organic layer and the post-extraction aliquot(s) are combined anddried, e.g., with MgSO₄ or Na₂SO₄, and the solvent is removed, e.g.,under reduced pressure, to provide a 1-heteroaromatic-piperidin-4-oneCompound of Formula 4 a-h which can be used without further purificationor, if desired, can be purified, e.g., using a silica gel column elutedwith 3:1 hexane:ethyl acetate.

In Step B2 of Scheme B, the 1-heteroaromatic-piperidin-4-one Compound ofFormula 4 a-h is reacted with a cyanation reagent, e.g., a cyanide saltsuch as NaCN, KCN or LiCN. In one embodiment, the present inventionrelates to a method for making a Cyclo(hetero)alkenyl Compoundcomprising allowing a 1-heteroaromatic-piperidin-4-one Compound ofFormula 4 a-h to react with a cyanation reagent. In another embodiment,the cyanide salt is NaCN, KCN, LiCN or a mixture thereof. In anotherembodiment, the cyanide salt is KCN. In another embodiment, the cyanidesalt is NaCN. In another embodiment, the cyanide salt is LiCN. Cyanidesalts are commercially available from, e.g., Aldrich Chemical Co.,Milwaukee, Wis., or can be prepared by methods known to those skilled inthe art.

In certain embodiments, the reaction in Step B2 is carried out with aninitial amount of cyanation reagent within the range of from about 1 toabout 4 equivalents, or within the range of from about 1.1 to about 2equivalents, on a molar basis, relative to the Compound of Formula 4a-h. In another embodiment, this reaction is carried out with about 1.2equivalents, on a molar basis, of cyanation reagent, relative to theCompound of Formula 4 a-h.

In certain embodiments, the Compound of Formula 4 a-h is present in thereaction in Step B2 at an initial concentration within the range of fromabout 0.05M to about 10M, or at an initial concentration within therange of from about 0.1M to about 5M. In a specific embodiment, theCompound of Formula 4 a-h is present in the reaction at an initialconcentration of about 0.3M.

In certain embodiments, the reaction in Step B2 is carried out at atemperature within the range of from about 0° C. to about 100° C.; at atemperature within the range of from about 0° C. to about 60° C.; or ata temperature within the range of from about 0° C. to about 25° C.

In certain embodiments, the reaction in Step B2 is carried out in apolar protic solvent, such as water, an alcohol, e.g., methanol, anorganic acid, e.g., acetic acid, an amide, e.g., formamide, orcombinations thereof. In one embodiment, the polar protic solvent iswater, methanol or combinations thereof. In another embodiment, thepolar protic solvent is water. In another embodiment, the polar proticsolvent is methanol. In other embodiments, the solvent comprises amixture of water and a suitable aprotic solvent or solvents, such asacetone, MEK, ethyl acetate, acetonitrile, dioxane,N-methyl-pyrrolidone, DMF, DMAc, DMSO, pyridine, and combinationsthereof. In such embodiments the ratio of water to aprotic solvent canbe within the range of from about 10:1 to about 1:1 (water:aproticsolvent). In certain embodiments, the aprotic solvent mixed with wateris selected from acetone, MEK, ethyl acetate, acetonitrile, dioxane,N-methyl-pyrrolidone, DMF, DMAc, DMSO, pyridine, and combinationsthereof.

In certain embodiments, the Compound of Formula 4 a-h is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with thecyanide salt. For example, the hydrochloride salt of the Compound ofFormula 4 a-h is dissolved in a suitable organic solvent, such as butnot limited to chloroform, to provide a solution that is extracted with,e.g., a saturated aqueous solution of Na₂CO₃. The organic layer isrecovered and the aqueous layer back-extracted with an additional volumeof the organic solvent. The organic solvent layers are combined,extracted with water, dried, e.g., over anhydrous sodium sulfate, andthen the liquid is removed to provide the Compound of Formula 4 a-h asthe free amine.

The reaction in Step B2 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step B2 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step B2 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step B2 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step B2 is carried out under an argonatmosphere.

Progress of the reaction in Step B2 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step B2 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a Compound ofFormula 11 a-h, to starting material, the Compound of Formula 4 a-h,remains essentially constant. Typically, a time sufficient for thereaction in Step B2 is within the range of from about 0.5 hours to about36 hours, from about 1 hour to about 24 hours, or from about 4 hours toabout 16 hours. In a specific embodiment, the reaction according to StepB2 is carried out for about 12 hours.

In another embodiment, the reaction according to Step B2 is carried outin water with about 1.2 equivalents, on a molar basis, of a cyanidesalt, relative to the Compound of Formula 4 a-h, at a temperature withinthe range of from about 0° C. to about 25° C. for a period of about 12hours with stirring.

Thereafter, the solvent is removed, e.g., under reduced pressure, toprovide a residue that can be purified, e.g., using a silica gel columneluted with 3:1 hexane:ethyl acetate, to provide a1-heteroaromatic-4-hydroxy-piperidine-4-carbonitrile Compound of Formula11 a-h. A Compound of Formula 11 a-h is useful, e.g., as an intermediatefor the synthesis of a Cyclo(hetero)alkenyl Compound.

In Step B3 of Scheme B, the1-heteroaromatic-4-hydroxy-piperidine-4-carbonitrile Compound of Formula11 a-h is reacted with a dehydrogenation agent, e.g., POCl₃, PSCl₃,PCl₅, SOCl₂ or COCl₂. In one embodiment, the present invention relatesto a method for making a Cyclo(hetero)alkenyl Compound comprisingallowing a 1-heteroaromatic-4-hydroxy-piperidine-4-carbonitrile Compoundof Formula 11 a-h to react with a dehydrogenation agent. In anotherembodiment, the dehydrogenation agent is POCl₃, PSCl₃, PCl₅, SOCl₂,COCl₂ or a mixture thereof. In another embodiment, the dehydrogenationagent is POCl₃, PSCl₃, SOCl₂ or a mixture thereof. In anotherembodiment, the dehydrogenation agent is POCl₃, PSCl₃ or a mixturethereof. In another embodiment, the dehydrogenation agent is POCl₃. Inanother embodiment, the dehydrogenation agent is PSCl₃. In anotherembodiment, the dehydrogenation agent is SOCl₂. In another embodiment,the dehydrogenation agent is COCl₂.

Such dehydrogenation agents are commercially available from, e.g.,Aldrich Chemical Co., or can be prepared by methods known to thoseskilled in the art.

In certain embodiments, the reaction in Step B3 is carried out with aninitial amount of dehydrogenation agent within the range of from about 1to about 10 equivalents, or within the range of from about 1.5 to about4 equivalents, on a molar basis, relative to the Compound of Formula 11a-h. In another embodiment, this reaction is carried out with about 2.2equivalents, on a molar basis, of dehydrogenation agent, relative to theCompound of Formula 11 a-h.

In certain embodiments, the Compound of Formula 11 a-h is present in thereaction in Step B3 at an initial concentration within the range of fromabout 0.05M to about 10M, or at an initial concentration within therange of from about 0.1M to about 2M. In a specific embodiment, theCompound of Formula 11 a-h is present in the reaction at an initialconcentration of about 0.25M.

In certain embodiments, the reaction in Step B3 is carried out at atemperature within the range of from about 0° C. to about 100° C.; at atemperature within the range of from about 0° C. to about 60° C.; or ata temperature within the range of from about 15° C. to about 30° C.

In certain embodiments, the reaction in Step B3 is carried out in anaprotic solvent, e.g., acetone, MEK, ethyl acetate, acetonitrile,dioxane, N-methyl-pyrrolidone, DMF, DMAc, DMSO, pyridine, andcombinations thereof. In one embodiment, the aprotic solvent ispyridine, dioxane or combinations thereof. In another embodiment, theaprotic solvent is pyridine. In another embodiment, the aprotic solventis dioxane.

In certain embodiments, the Compound of Formula 11 a-h is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with thedehydrogenation agent. For example, the hydrochloride salt of theCompound of Formula 11 a-h is dissolved in a suitable organic solvent,such as but not limited to chloroform, to provide a solution that isextracted with, e.g., a saturated aqueous solution of Na₂CO₃. Theorganic layer is recovered and the aqueous layer back-extracted with anadditional volume of the organic solvent. The organic solvent layers arecombined, extracted with water, dried, e.g., over anhydrous sodiumsulfate, and then the liquid is removed to provide the Compound ofFormula 11 a-h as the free amine.

The reaction in Step B3 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step B3 iscarried out in an inert atmosphere. In one non-limiting aspect of thisembodiment, the reaction in Step B3 is carried out under a nitrogenatmosphere. In another non-limiting aspect of this embodiment, thereaction in Step B3 is carried out under an argon atmosphere.

Progress of the reaction in Step B3 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step B3 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a Compound ofFormula 12 a-h, to starting material, the Compound of Formula 11 a-h,remains essentially constant. Typically, a time sufficient for thereaction in Step B3 is within the range of from about 0.5 hours to about48 hours, from about 2 hours to about 36 hours, or from about 4 hours toabout 24 hours. In a specific embodiment, the reaction according to StepB3 is carried out for about 22 hours.

In another embodiment, the reaction according to Step B3 is carried outin pyridine with about 2.2 equivalents, on a molar basis, of adehydrogenation agent, relative to the Compound of Formula 11 a-h, at atemperature within the range of from about 20° C. to about 25° C. for aperiod of about 22 hours with stirring.

Thereafter, the solvent is removed, e.g., under reduced pressure, toprovide a residue that can be purified, e.g., using a silica gel columneluted with 5:1 hexane:ethyl acetate, to provide a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonitrile Compound ofFormula 12 a-h. A Compound of Formula 12 a-h is useful, e.g., as anintermediate for the synthesis of a Cyclo(hetero)alkenyl Compound.

In Step B4 of Scheme B, the1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonitrile Compound ofFormula 12 a-h is reacted with an acidifying reagent, e.g., an inorganicacid such as HCl or H₂SO₄, or an organic acid, such as phthalic acid ortetrahalophthalic acid. In one embodiment, the present invention relatesto a method for making a Cyclo(hetero)alkenyl Compound comprisingallowing a 1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonitrileCompound of Formula 12 a-h to react with an acidifying reagent. Inanother embodiment, the acidifying reagent is HCl, H₂SO₄, phthalic acid,tetrahalophthalic acid or a mixture thereof. In another embodiment, theacidifying reagent is HCl. In another embodiment, the acidifying reagentis H₂SO₄. In another embodiment, the acidifying reagent is phthalicacid. In another embodiment, the acidifying reagent is tetrahalophthalicacid.

In certain embodiments, the acidifying reagent is present in thereaction in Step B4 at an initial concentration within the range of fromabout 0.5N to about 12N, or at an initial concentration within the rangeof from about 1N to about 8N. In a specific embodiment, the acidifyingreagent is present in the reaction at an initial concentration of about6N.

In certain embodiments, the Compound of Formula 12 a-h is present in thereaction in Step B4 at an initial concentration within the range of fromabout 0.05M to about 10M, or at an initial concentration within therange of from about 0.1M to about 5M. In a specific embodiment, theCompound of Formula 12 a-h is present in the reaction at an initialconcentration of about 0.5M.

In certain embodiments, the reaction in Step B4 is carried out at atemperature within the range of from about 0° C. to about 120° C.; at atemperature within the range of from about 25° C. to about 120° C.; orat a temperature within the range of from about 95° C. to about 105° C.

In certain embodiments, the reaction in Step B4 is carried out in apolar protic solvent or in combinations of such solvents; polar proticsolvents have been described above. In one embodiment, the polar proticsolvent is water, an organic acid, e.g., formic acid (see U.S. Pat. No.5,206,392) or combinations thereof. In another embodiment, the polarprotic solvent is water. In other embodiments, the solvent comprises amixture of water and a suitable aprotic solvent or solvents. In suchembodiments the ratio of water to aprotic solvent can be within therange of from about 10:1 to about 1:1 (water:aprotic solvent). Incertain embodiments, the aprotic solvent mixed with water is selectedfrom acetone, MEK, ethyl acetate, acetonitrile, dioxane,N-methyl-pyrrolidone, DMF, DMAc, DMSO, pyridine, and combinationsthereof.

In certain embodiments, the Compound of Formula 12 a-h is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with theacidifying reagent. For example, the hydrochloride salt of the Compoundof Formula 12 a-h is dissolved in a suitable organic solvent, such asbut not limited to chloroform, to provide a solution that is extractedwith, e.g., a saturated aqueous solution of Na₂CO₃. The organic layer isrecovered and the aqueous layer back-extracted with an additional volumeof the organic solvent. The organic solvent layers are combined,extracted with water, dried, e.g., over anhydrous sodium sulfate, andthen the liquid is removed to provide the Compound of Formula 12 a-h asthe free amine.

The reaction in Step B4 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step B4 iscarried out in an inert atmosphere. In one non-limiting aspect of thisembodiment, the reaction in Step B4 is carried out under a nitrogenatmosphere. In another non-limiting aspect of this embodiment, thereaction in Step B4 is carried out under an argon atmosphere.

Progress of the reaction in Step B4 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step B4 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a Compound ofFormula 13 a-h, to starting material, the Compound of Formula 12 a-h,remains essentially constant. Typically, a time sufficient for thereaction in Step B4 is within the range of from about 0.5 hours to about36 hours, from about 1 hour to about 24 hours, or from about 4 hours toabout 16 hours. In a specific embodiment, the reaction according to StepB4 is carried out for about 12 hours.

In another embodiment, the reaction according to Step B4 is carried outin water with about a 6N initial concentration of HCl, at a temperaturewithin the range of from about 95° C. to about 105° C., and for a periodof about 12 hours with refluxing.

The resulting reaction mixture is cooled to about 25° C. and the solventis removed, e.g., under reduced pressure, to provide a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid Compoundof Formula 13 a-h, which can be used without further purification or, ifdesired, can be purified using methods known to those skilled in theart. A Compound of Formula 13 a-h is useful, e.g., as an intermediatefor the synthesis of a Cyclo(hetero)alkenyl Compound.

In Step B5 of Scheme B, the1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid Compoundof Formula 13 a-h is reacted in a single step procedure with a compoundof formula Ar²—NHR₄. In one embodiment, the present invention relates toa method for making a Cyclo(hetero)alkenyl Compound comprising allowinga 1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acidCompound of Formula 13 a-h to react with a compound of formula Ar²—NHR₄.In another embodiment, this reaction is in a single step. In anotherembodiment, the compound of formula Ar²—NHR₄ is4-trifluoromethyl-aniline. In another embodiment, the compound offormula Ar²—NHR₄ is 5-trifluoromethyl-pyridin-2-ylamine. In anotherembodiment, the compound of formula Ar²—NHR₄ is2,2-difluoro-benzo[1,3]dioxol-5-ylamine. Ar²—NHR₄ compounds arecommercially available from, e.g., Aldrich Chemical Co., or can beprepared by methods known to those skilled in the art.

In certain embodiments, the reaction in Step B5 is carried out with aninitial amount of the a compound of formula Ar²—NHR₄ within the range offrom about 1 to about 5 equivalents, or within the range of from about 1to about 2 equivalents, on a molar basis, relative to the Compound ofFormula 13 a-h. In another embodiment, this reaction is carried out withabout 1 equivalent, on a molar basis, of the compound of formulaAr²—NHR₄, relative to the Compound of Formula 13 a-h.

In certain embodiments, the reaction in Step B5 is carried out toinclude an initial amount of 1-hydroxybenzotriazole (HOBt) within therange of from about 0.1 to about 3 equivalents, or within the range offrom about 0.2 to about 1.5 equivalents, on a molar basis, relative tothe Compound of Formula 13 a-h. In another embodiment, this reaction iscarried out with about 1.25 equivalents, on a molar basis, of HOBt,relative to the Compound of Formula 13 a-h.

In certain embodiments, the reaction in Step B5 is carried out toinclude an initial amount of DIC within the range of from about 0.1 toabout 3 equivalents, or within the range of from about 0.2 to about 1.5equivalents, on a molar basis, relative to the Compound of Formula 13a-h. In another embodiment, this reaction is carried out with about 1.25equivalents, on a molar basis, of DIC, relative to the Compound ofFormula 13 a-h. In another embodiment, this reaction is carried out toinclude an initial amount of DIC about identical with the initial amountof HOBt, each on a molar basis relative to the Compound of Formula 13a-h. HOBt and DIC are commercially available from, e.g., AldrichChemical Co., or can be prepared by methods known to those skilled inthe art.

In certain embodiments, the Compound of Formula 13 a-h is present in thereaction in Step B5 at an initial concentration within the range of fromabout 0.05M to about 10M, or at an initial concentration within therange of from about 0.1M to about 1M. In a specific embodiment, theCompound of Formula 13 a-h is present in the reaction at an initialconcentration of about 0.35M.

In certain embodiments, the reaction in Step B5 is carried out at atemperature within the range of from about 0° C. to about 100° C.; at atemperature within the range of from about 0° C. to about 60° C.; or ata temperature within the range of from about 15° C. to about 30° C.

In certain embodiments, the reaction in Step B5 is carried out in anaprotic solvent or in combinations of such solvents; aprotic solventshave been described above. In one embodiment, the aprotic solvent ispyridine, DMF or combinations thereof. In another embodiment, theaprotic solvent is DMF. In another embodiment, the aprotic solvent ispyridine.

In certain embodiments, the Compound of Formula 13 a-h is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with thecompound of formula Ar²—NHR₄. For example, the hydrochloride salt of theCompound of Formula 13 a-h is dissolved in a suitable organic solvent,such as but not limited to chloroform, to provide a solution that isextracted with, e.g., a saturated aqueous solution of Na₂CO₃. Theorganic layer is recovered and the aqueous layer back-extracted with anadditional volume of the organic solvent. The organic solvent layers arecombined, extracted with water, dried, e.g., over anhydrous sodiumsulfate, and then the liquid is removed to provide the Compound ofFormula 13 a-h as the free amine.

The reaction in Step B5 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step B5 iscarried out in an inert atmosphere. In one non-limiting aspect of thisembodiment, the reaction in Step B5 is carried out under a nitrogenatmosphere. In another non-limiting aspect of this embodiment, thereaction in Step B5 is carried out under an argon atmosphere.

Progress of the reaction in Step B5 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step B5 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, theCyclo(hetero)alkenyl Compound, to starting material, the Compound ofFormula 13 a-h, remains essentially constant. Typically, a timesufficient for the reaction in Step B5 is within the range of from about0.5 hours to about 36 hours, from about 1 hour to about 24 hours, orfrom about 4 hours to about 16 hours. In a specific embodiment, thereaction according to Step B5 is carried out for about 12 hours.

In another embodiment, the reaction according to Step B5 is carried outin DMF with about 1 equivlent of a compound of formula Ar²—NHR₄,1-hydroxybenzotriazole (HOBt, about 1.25 eq.), and DIC (about 1.25 eq.)relative to the Compound of Formula 13 a-h (present at an initialconcentration of about 0.35M), at a temperature within the range of fromabout 20° C. to about 25° C. for a period of about 12 hours withstirring.

Thereafter, the solvent is removed, e.g., under reduced pressure, toprovide a residue that can be purified, e.g., using a silica gel columneluted with 10:1 hexane:ethyl acetate, to provide a Cyclo(hetero)alkenylCompound where V is N. Where m=1, a mixture of Cyclo(hetero)alkenylCompounds where V is N is generally obtained. The mixture can beseparated by conventional methods, for example, column chromatography.

A Cyclo(hetero)alkenyl Compound where V is N can also be obtained from aCompound of Formula 13 a-h by a two-step procedure, e.g., Step B6followed by Step B7. In one embodiment, the present invention relates toa method for making a Cyclo(hetero)alkenyl Compound comprising allowinga 1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acidCompound of Formula 13 a-h to react, in a plurality of steps; in onestep the reacting is with a compound of formula Ar²—NHR₄.

In Step B6 of Scheme B, the1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid Compoundof Formula 13 a-h is reacted with an excess of a Lewis acid comprisingchlorine, such as SOCl₂, COCl₂, PSCl₃, PCl₅ or POCl₃, which serves as areagent and can also serve as a solvent. In one embodiment, the presentinvention relates to a method for making a Cyclo(hetero)alkenyl Compoundcomprising allowing a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid Compoundof Formula 13 a-h to react with an excess of a Lewis acid comprisingchlorine. In another embodiment, the Lewis acid comprising chlorine isPOCl₃, PSCl₃, PCl₅, SOCl₂, COCl₂ or a mixture thereof. In anotherembodiment, the Lewis acid comprising chlorine is SOCl₂, COCl₂ or amixture thereof. In another embodiment, the Lewis acid comprisingchlorine is SOCl₂. In another embodiment, the Lewis acid comprisingchlorine is POCl₃. In another embodiment, the Lewis acid comprisingchlorine is COCl₂.

In certain embodiments, the reaction in Step B6 is carried out with aninitial amount of the Lewis acid within the range of from about 1 toabout 100 equivalents, or within the range of from about 1 to about 50equivalents, on a molar basis, relative to the Compound of Formula 13a-h. In another embodiment, this reaction is carried out with about 24equivalents, on a molar basis, of the Lewis acid, relative to theCompound of Formula 13 a-h.

In certain embodiments, the Compound of Formula 13 a-h is present in thereaction in Step B6 at an initial concentration within the range of fromabout 0.05M to about 10M, or at an initial concentration within therange of from about 0.1M to about 5M. In a specific embodiment, theCompound of Formula 13 a-h is present in the reaction at an initialconcentration of about 0.6M.

In certain embodiments, the reaction in Step B6 is carried out at atemperature within the range of from about 0° C. to about 100° C.; at atemperature within the range of from about 10° C. to about 60° C.; or ata temperature within the range of from about 15° C. to about 30° C.

In certain embodiments, the reaction in Step B6 is carried out in anonpolar solvent, e.g., THF, an aprotic solvent or in combinations ofsuch solvents; nonpolar solvents and aprotic solvents have beendescribed above. In certain embodiments, the reaction in Step B6 iscarried out without a solvent, i.e., the Lewis acid serves as thesolvent. In another embodiment, the solvent is THF. In anotherembodiment, the solvent is SOCl₂. In another embodiment, the solvent isPOCl₃. In another embodiment, the solvent is COCl₂.

In certain embodiments, the Compound of Formula 13 a-h is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with theLewis acid. For example, the hydrochloride salt of the Compound ofFormula 13 a-h is dissolved in a suitable organic solvent, such as butnot limited to chloroform, to provide a solution that is extracted with,e.g., a saturated aqueous solution of Na₂CO₃. The organic layer isrecovered and the aqueous layer back-extracted with an additional volumeof the organic solvent. The organic solvent layers are combined,extracted with water, dried, e.g., over anhydrous sodium sulfate, andthen the liquid is removed to provide the Compound of Formula 13 a-h asthe free amine.

The reaction in Step B6 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step B6 iscarried out in an inert atmosphere. In one non-limiting aspect of thisembodiment, the reaction in Step B6 is carried out under a nitrogenatmosphere. In another non-limiting aspect of this embodiment, thereaction in Step B6 is carried out under an argon atmosphere.

Progress of the reaction in Step B6 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step B6 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a Compound ofFormula 14 a-h, to starting material, the Compound of Formula 13 a-h,remains essentially constant. Typically, a time sufficient for thereaction in Step B6 is within the range of from about 0.5 hours to about36 hours, from about 1 hour to about 24 hours, or from about 4 hours toabout 19 hours. In a specific embodiment, the reaction according to StepB6 is carried out for about 12 hours. In a specific embodiment, thereaction according to Step B6 is carried out for about 17 hours.

In another embodiment, the reaction according to Step B6 is carried outby reacting the Compound of Formula 13 a-h (about 1 eq.) with an excessof a Lewis acid comprising chlorine (about 24 eq.), at a temperature ofabout 25° C. for a period of about 12 hours with stirring to provide a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonyl chlorideCompound of Formula 14 a-h, which can be used without furtherpurification or, if desired, can be purified using methods known tothose skilled in the art. A Compound of Formula 14 a-h is useful, e.g.,as an intermediate for the synthesis of a Cyclo(hetero)alkenyl Compound.

In Step B7 of Scheme B, the1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonyl chlorideCompound of Formula 14 a-h is reacted with a compound of formulaAr²—NHR₄. In one embodiment, the present invention relates to a methodfor making a Cyclo(hetero)alkenyl Compound comprising allowing a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonyl chlorideCompound of Formula 14 a-h to react with a compound of formula Ar²—NHR₄.In another embodiment, the compound of formula Ar²—NHR₄ is4-trifluoromethyl-aniline. In another embodiment, the compound offormula Ar²—NHR₄ is 5-trifluoromethyl-pyridin-2-ylamine. In anotherembodiment, the compound of formula Ar²—NHR₄ is2,2-difluoro-benzo[1,3]dioxol-5-ylamine.

In certain embodiments, the reaction in Step B7 is carried out with aninitial amount of the a compound of formula Ar²—NHR₄ within the range offrom about 1 to about 10 equivalents, or within the range of from about1 to about 5 equivalents, on a molar basis, relative to the Compound ofFormula 14 a-h. In another embodiment, this reaction is carried out withabout 1.5 equivalents, on a molar basis, of the compound of formulaAr²—NHR₄, relative to the Compound of Formula 14 a-h. In anotherembodiment, this reaction is carried out with about 1.2 equivalents, ona molar basis, of the compound of formula Ar²—NHR₄, relative to theCompound of Formula 14 a-h. In another embodiment, this reaction iscarried out with about 1.1 equivalents, on a molar basis, of thecompound of formula Ar²—NHR₄, relative to the Compound of Formula 14a-h.

In certain embodiments, the reaction in Step B7 is carried out toinclude an initial amount of an organic base, an inorganic base or amixture thereof. In certain embodiments, the reaction in Step B7 iscarried out to include an initial amount of an organic base, e.g.,pyridine or a trialkylamine, such as triethylamine, trimethylamine,methyl diethylamine or diisopropyl ethylamine, within the range of fromabout 1 to about 5 equivalents, or within the range of from about 1 toabout 2 equivalents, on a molar basis, relative to the Compound ofFormula 14 a-h. In another embodiment, this reaction is carried out withabout 1.25 equivalents, on a molar basis, of organic base, e.g.,trialkylamine, relative to the Compound of Formula 14 a-h. In oneembodiment, the trialkylamine is triethylamine, trimethylamine, methyldiethylamine, diisopropyl ethylamine or combinations thereof. In anotherembodiment, the trialkylamine is triethylamine. Trialkylamines arecommercially available from, e.g., Aldrich Chemical Co., or can beprepared by methods known to those skilled in the art.

In certain embodiments, the reaction in Step B7 is carried out toinclude an initial amount of an inorganic base, such as sodiumbicarbonate, within the range of from about 1 to about 10 equivalents,or within the range of from about 1 to about 5 equivalents, on a molarbasis, relative to the Compound of Formula 14 a-h. In anotherembodiment, this reaction is carried out with about 3 equivalents, on amolar basis, of inorganic base, relative to the Compound of Formula 14a-h. In one embodiment, the inorganic base is sodium bicarbonate, sodiumcarbonate, potassium bicarbonate, potassium carbonate or combinationsthereof. In another embodiment, the inorganic base is sodiumbicarbonate. In another embodiment, the inorganic base is potassiumcarbonate.

In certain embodiments, the Compound of Formula 14 a-h is present in thereaction in Step B7 at an initial concentration within the range of fromabout 0.05M to about 10M, at an initial concentration within the rangeof from about 0.1M to about 5M, at an initial concentration within therange of from about 0.1M to about 2M. In a specific embodiment, theCompound of Formula 14 a-h is present in the reaction at an initialconcentration of about 0.2M. In a specific embodiment, the Compound ofFormula 14 a-h is present in the reaction at an initial concentration ofabout 0.3M. In a specific embodiment, the Compound of Formula 14 a-h ispresent in the reaction at an initial concentration of about 0.5M.

In certain embodiments, the reaction in Step B7 is carried out at atemperature within the range of from about 0° C. to about the boilingpoint of the solvent; at a temperature within the range of from about 0°C. to about 115° C.; at a temperature within the range of from about 0°C. to about 100° C.; at a temperature within the range of from about 0°C. to about 80° C.; at a temperature within the range of from about 40°C. to about 80° C.; or at a temperature within the range of from about15° C. to about 30° C.

In certain embodiments, the reaction in Step B7 is carried out in anaprotic solvent or in combinations of such solvents; aprotic solventshave been described above. In one embodiment, the aprotic solvent isDCM, DCE, THF, pyridine or combinations thereof. In another embodiment,the aprotic solvent is DCM. In another embodiment, the aprotic solventis DCE. In another embodiment, the aprotic solvent is THF. In anotherembodiment, the aprotic solvent is pyridine. As pyridine can serve in adual role, i.e., simultaneously serve as a solvent and as an organicbase, as discussed above, if such a dual-role organic base is presentthen the reaction in Step B7 is carried out, in certain embodiments,with an initial amount of the dual-role organic base within the range offrom about 1 to about 100 equivalents, or within the range of from about1 to about 50 equivalents, on a molar basis, relative to the Compound ofFormula 14 a-h.

In certain embodiments, the Compound of Formula 14 a-h is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with thecompound of formula Ar²—NHR₄. For example, the hydrochloride salt of theCompound of Formula 14 a-h is dissolved in a suitable organic solvent,such as but not limited to chloroform, to provide a solution that isextracted with, e.g., a saturated aqueous solution of Na₂CO₃. Theorganic layer is recovered and the aqueous layer back-extracted with anadditional volume of the organic solvent. The organic solvent layers arecombined, extracted with water, dried, e.g., over anhydrous sodiumsulfate, and then the liquid is removed to provide the Compound ofFormula 14 a-h as the free amine.

The reaction in Step B7 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step B7 iscarried out in an inert atmosphere. In one non-limiting aspect of thisembodiment, the reaction in Step B7 is carried out under a nitrogenatmosphere. In another non-limiting aspect of this embodiment, thereaction in Step B7 is carried out under an argon atmosphere.

Progress of the reaction in Step B7 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step B7 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, theCyclo(hetero)alkenyl Compound, to starting material, the Compound ofFormula 14 a-h, remains essentially constant. Typically, a timesufficient for the reaction in Step B7 is within the range of from about0.5 hours to about 24 hours; from about 1 hour to about 19 hours; orfrom about 1 hour to about 17 hours. In a specific embodiment, thereaction according to Step B7 is carried out for about 1.6 hours. In aspecific embodiment, the reaction according to Step B7 is carried outfor about 4 hours. In a specific embodiment, the reaction according toStep B7 is carried out for about 16 hours.

In another specific embodiment, the reaction according to Step B7 iscarried out in DCM with about 1.5 equivalents of a compound of formulaAr²—NHR₄ and a trialkylamine, such as triethylamine, trimethylamine,methyl diethylamine or diisopropyl ethylamine (about 2.0 eq.) relativeto the Compound of Formula 14 a-h (present at an initial concentrationof about 0.2M). The resulting solution is degassed by bubbling nitrogenthrough the solution. The reaction mixture is kept at a temperaturewithin the range of from about 20° C. to about 25° C. for a period ofabout 4 hours with stirring.

In another specific embodiment, the reaction according to Step B7 iscarried out in pyridine with about 1.2 equivalents of a compound offormula Ar²—NHR₄ relative to the Compound of Formula 14 a-h (present atan initial concentration of about 0.5M). For example, a 0.5M suspensionof the Compound of Formula 14 a-h in pyridine can be added to a 0.5Msolution of a compound of formula Ar²—NHR₄ in pyridine about 25° C. toform a reaction mixture and the reaction mixture is kept at atemperature of about 70° C. for a period of about 16 hours withstirring.

In another specific embodiment, the reaction according to Step B7 iscarried out in THF at about 0° C. with about 1.1 equivalents of acompound of formula Ar²—NHR₄ and a base, such as sodium bicarbonate(about 3.0 eq.) relative to the Compound of Formula 14 a-h (present atan initial concentration of about 0.3M). The resulting solution isstirred at 0° C. for about 5 min, warmed to about 25° C. over a periodof about 30 min with stirring, and kept at about 65° C. for 1 hour withstirring. Thereafter, the solvent is removed, e.g., under reducedpressure, to provide a residue that suspended in ethyl acetate andwashed with aqueous 3N HCl such that separate aqueous and organic layersform. The layers can be separated and the aqueous layer extracted withethyl acetate as required. The organic layer can be combined with thepost-extraction ethyl acetate aliquot(s) and the combination dried,e.g., with Na₂SO₄.

Thereafter, in any of these specific embodiments for conducting thereaction according to Step B7, the solvent is removed, e.g., underreduced pressure, to provide a residue that can be purified, e.g., usinga silica gel column eluted with 10:1 hexane:ethyl acetate or using flashchromatography on a silica gel column with 1:1 (by volume) ethylacetate:hexane as an eluent, to provide a Cyclo(hetero)alkenyl Compoundwhere V is N. As discussed above, if a mixture of Cyclo(betero)alkenylCompounds is obtained where m=1, the mixture can be separated byconventional methods, for example, column chromatography.

The Compound of Formula (I) where X is S can be made by, e.g., reactinga Compound of Formula (II) (i.e., where X is O) with Lawesson's reagentas described in connection with Scheme A. In another embodiment, theCompound of Formula (I) where X is S can be made by forming a dithioacid from the Compound of Formula 13 a-h, e.g., according to theprocedure described in Helvetica Chimica Acta 3:824-33 (1920). Thedithio acid can be reacted according to Step B5 of Scheme B or accordingto the two-step procedure of Scheme B, e.g., Step B6 followed by StepB7, as described above.

Thus, in another embodiment, a method for preparing aCyclo(hetero)alkenyl Compound comprises allowing a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid compoundto react with a compound of formula Ar²—NHR₄ to provide theCyclo(hetero)alkenyl Compound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises forming the Cyclo(hetero)alkenyl Compound from the1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid compoundin one step.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises forming the Cyclo(hetero)alkenyl Compound from the1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid compoundin a plurality of steps.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises:

(i) allowing a 1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylicacid compound to react with a Lewis acid comprising chlorine in a firststep to provide a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonyl chloridecompound; and

(ii) allowing the1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonyl chloridecompound to react with the compound of formula Ar²—NHR₄ in a second stepto provide a Cyclo(hetero)alkenyl Compound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-cabonitrile compound toreact with an acidifying reagent to provide a 1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid compound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing a1-heteroaromatic-4-hydroxy-piperidine-4-carbonitrile compound to reactwith a dehydrogenation agent to provide a1-heteroaromatic-1,2,3,6-tetrahydro-pyridine-4-carbonitrile compound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing a 1-heteroaromatic-piperidin-4-one compoundto react with a cyanation reagent to provide the1-heteroaromatic-4-hydroxy-piperidine-4-carbonitrile compound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing a8-heteroaromatic-1,4-dioxa-8-aza-spiro[4.5]decane compound to react witha ketone-forming reagent to provide a 1-heteroaromatic-piperidin-4-onecompound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing a8-heteroaromatic-1,4-dioxa-8-aza-spiro[4.5]decane compound to react witha ketone-forming reagent to provide the 1-heteroaromatic-piperidin-4-onecompound.

In another embodiment, the present invention relates to a compound offormula 4 a-h

or a pharmaceutically acceptable salt thereof, where:

Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo);

each R₂ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to        10-membered)heteroaryl, each of which is unsubstituted or        substituted with one or more R₆ groups;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, NO₂, —N(R₇)₂, —CH═NR₇, NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

n is an integer ranging from 0 to 3; and

p is an integer ranging from 0 to 2.

In another embodiment, the present invention relates to a compound offormula 11 a-h

or a pharmaceutically acceptable salt thereof, where:

Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo);

each R₂ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to        10-membered)heteroaryl, each of which is unsubstituted or        substituted with one or more R₆ groups;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

n is an integer ranging from 0 to 3; and

p is an integer ranging from 0 to 2.

In another embodiment, the present invention relates to a compound offormula 12 a-h

or a pharmaceutically acceptable salt thereof, where:

Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —H, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo);

each R₂ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to        10-membered)heteroaryl, each of which is unsubstituted or        substituted with one or more R₆ groups;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

n is an integer ranging from 0 to 3; and

p is an integer ranging from 0 to 2.

In another embodiment, the present invention relates to a compound offormula 13 a-h

or a pharmaceutically acceptable salt thereof, where:

Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo);

each R₂ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,        —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl,        —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl,        —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or        -(7- to 10-membered)bicycloheterocycle, each of which is        unsubstituted or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to        10-membered)heteroaryl, each of which is unsubstituted or        substituted with one or more R₆ groups;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

n is an integer ranging from 0 to 3; and

p is an integer ranging from 0 to 2.

In another embodiment, the present invention relates to a compound offormula 14 a-h

or a pharmaceutically acceptable salt thereof, where:

Ar¹ is

R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo);

each R₂ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to        10-membered)heteroaryl, each of which is unsubstituted or        substituted with one or more R₆ groups;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

n is an integer ranging from 0 to 3; and

p is an integer ranging from 0 to 2.

In another embodiment, the present invention relates to methods formaking the Cyclo(hetero)alkenyl Compounds where V is N from the aminoCompounds of Formula 17 a-l and the isonicotinoyl chloride Compounds ofFormula 16 by the following non-limiting illustrative method shown belowin Scheme C.

where R₃, R₄, R₈, R₉, Y, Ar¹, Ar², m, q, r and s are defined above and Zis Cl, Br or I.

In Step C1 of Scheme C, the isonicotinic acid Compound of Formula 15,which can be obtained, for example, commercially from, e.g., AldrichChemical Co., or can be prepared by methods known to those skilled inthe art, is reacted with an excess of a Lewis acid comprising chlorine,such as SOCl₂, COCl₂, PSCl₃, PCl₅ or POCl₃, which serves as a reagentand can also serve as a solvent. In one embodiment, the presentinvention relates to a method for making a Cyclo(hetero)alkenyl Compoundcomprising allowing an isonicotinic acid Compound of Formula 15 to reactwith an excess of a Lewis acid comprising chlorine. In anotherembodiment, the Lewis acid comprising chlorine is POCl₃, PSCl₃, PCl₅,SOCl₂, COCl₂ or a mixture thereof. In another embodiment, the Lewis acidcomprising chlorine is SOCl₂, COCl₂ or a mixture thereof. In anotherembodiment, the Lewis acid comprising chlorine is SOCl₂. In anotherembodiment, the Lewis acid comprising chlorine is POCl₃. In anotherembodiment, the Lewis acid comprising chlorine is COCl₂.

In certain embodiments, the reaction in Step C1 is carried out with aninitial amount of the Lewis acid within the range of from about 1 toabout 30 equivalents, or within the range of from about 1 to about 20equivalents, on a molar basis, relative to the Compound of Formula 15.In another embodiment, this reaction is carried out with about 11equivalents, on a molar basis, of the Lewis acid, relative to theCompound of Formula 15.

In certain embodiments, the Compound of Formula 15 is present in thereaction in Step C1 at an initial concentration within the range of fromabout 1M to about 4M, or at an initial concentration within the range offrom about 1M to about 2M. In a specific embodiment, the Compound ofFormula 15 is present in the reaction at an initial concentration ofabout 1.2M.

In certain embodiments, the reaction in Step C1 is carried out at atemperature within the range of from about 10° C. to about 45° C.; at atemperature within the range of from about 10° C. to about 40° C.; or ata temperature within the range of from about 15° C. to about 30° C.

In certain embodiments, the reaction in Step C1 is carried out in anaprotic solvent, e.g., acetone, MEK, ethyl acetate, acetonitrile,dioxane, N-methyl-pyrrolidone, DMF, DMAc, DMSO, pyridine, DCM, DCE andcombinations thereof. In certain embodiments, the reaction in Step C1 iscarried out without a solvent, i.e., the Lewis acid serves as thesolvent. In another embodiment, the solvent is SOCl₂.

In certain embodiments, the Compound of Formula 15 is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with theLewis acid. For example, the hydrochloride salt of the Compound ofFormula 15 is dissolved in a suitable organic solvent, such as but notlimited to chloroform, to provide a solution that is extracted with,e.g., a saturated aqueous solution of Na₂CO₃. The organic layer isrecovered and the aqueous layer back-extracted with an additional volumeof the organic solvent. The organic solvent layers are combined,extracted with water, dried, e.g., over anhydrous sodium sulfate, andthen the liquid is removed to provide the Compound of Formula 15 as thefree amine.

The reaction in Step C1 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step C1 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step C1 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step C1 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step C1 is carried out under an argonatmosphere.

Progress of the reaction in Step C1 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step C1 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a Compound ofFormula 16, to starting material, the Compound of Formula 15, remainsessentially constant. Typically, a time sufficient for the reaction inStep C1 is within the range of from about 1 hour to about 48 hours, fromabout 5 hours to about 36 hours, or from about 10 hours to about 24hours. In a specific embodiment, the reaction according to Step C1 iscarried out for about 17 hours.

In another embodiment, the reaction according to Step C1 is carried outby reacting the Compound of Formula 15 (about 1 eq.) with an excess of aLewis acid comprising chlorine (about 11 eq.), at a temperature of about25° C. for a period of about 17 hours with stirring to provide anisonicotinolyl chloride Compound of Formula 16, which, after the Lewisacid comprising chlorine is removed, e.g., under reduced pressure, canbe used without further purification or, if desired, can be purified.For example, THF can be used to dissolve the Compound of Formula 16 andthe solvent can be removed, e.g., under reduced pressure, to provide apurified Compound of Formula 16.

In Step C2 of Scheme C, the isonicotinolyl chloride Compound of Formula16 is reacted with a compound of formula Ar²—NHR₄, e.g., a Compound ofFormula 17 a-l. In one embodiment, the present invention relates tomethod for making a Cyclo(hetero)alkenyl Compound comprising allowing anisonicotinolyl chloride Compound of Formula 16 to react with a compoundof formula Ar²—NHR₄. In another embodiment, the compound of formulaAr²—NHR₄ is 4-trifluoromethyl-aniline. In another embodiment, thecompound of formula Ar²—NHR₄ is 5-trifluoromethyl-pyridin-2-ylamine. Inanother embodiment, the compound of formula Ar²—NHR₄ is2,2-difluoro-benzo[1,3]dioxol-5-ylamine. In another embodiment, thecompound of formula Ar²—NHR₄ is 6-fluoro-benzothiazol-2ylamine.

In certain embodiments, the reaction in Step C2 is carried out with aninitial amount of the a compound of formula Ar²—NHR₄ within the range offrom about 1 to about 2 equivalents, or within the range of from about 1to about 1.5 equivalents, on a molar basis, relative to the Compound ofFormula 16. In another embodiment, this reaction is carried out withabout 1.1 equivalents, on a molar basis, of the compound of formulaAr²—NHR₄, relative to the Compound of Formula 16.

In certain embodiments, the Compound of Formula 16 is present in thereaction in Step C2 at an initial concentration within the range of fromabout 0.05M to about 2M, or at an initial concentration within the rangeof from about 0.1M to about 1M. In a specific embodiment, the Compoundof Formula 16 is present in the reaction at an initial concentration ofabout 0.3M.

In certain embodiments, the reaction in Step C2 is carried out toinclude an initial amount of a base, such as an inorganic base, e.g.,sodium bicarbonate, within the range of from about 1 to about 10equivalents, or within the range of from about 1 to about 5 equivalents,on a molar basis, relative to the Compound of Formula 16. In anotherembodiment, this reaction is carried out with about 3 equivalents, on amolar basis, of base, relative to the Compound of Formula 16. In oneembodiment, the inorganic base is sodium bicarbonate, sodium carbonate,potassium bicarbonate, potassium carbonate or combinations thereof. Inanother embodiment, the base is sodium bicarbonate. In anotherembodiment, the base is potassium carbonate.

In certain embodiments, the reaction in Step C2 is carried out at atemperature within the range of from about −10° C. to about 80° C.; at atemperature within the range of from about −10° C. to about 65° C.; orat a temperature within the range of from about 0° C. to about 65° C.

In certain embodiments, the reaction in Step C2 is carried out in anonpolar solvent, e.g., hexane, heptane, benzene, diethyl ether, THF,DCM, DCE, chloroform, carbon tetrachloride and combinations thereof. Inone embodiment, the nonpolar solvent is THF, DCM, DCE or combinationsthereof. In another embodiment, the nonpolar solvent is THF. In anotherembodiment, the nonpolar solvent is DCM.

In certain embodiments, the Compound of Formula 17 a-l is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction in Step C2.For example, the hydrochloride salt of the Compound of Formula 17 a-l isdissolved in a suitable organic solvent, such as but not limited tochloroform, to provide a solution that is extracted with, e.g., asaturated aqueous solution of Na₂CO₃. The organic layer is recovered andthe aqueous layer back-extracted with an additional volume of theorganic solvent. The organic solvent layers are combined, extracted withwater, dried, e.g., over anhydrous sodium sulfate, and then the liquidis removed to provide the Compound of Formula 17 a-l as the free amine.

The reaction in Step C2 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step C2 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step C2 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step C2 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step C2 is carried out under an argonatmosphere.

Progress of the reaction in Step C2 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step C2 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, theisonicotinamide Compound of Formula 18 a-l, to starting material, theCompound of Formula 16, remains essentially constant. Typically, a timesufficient for the reaction in Step C2 is within the range of from about5 minutes to about 5 hours, from about 5 minutes to about 3 hours, orfrom about 15 minutes to about 3 hours. In a specific embodiment, thereaction according to Step C2 is carried out for about 1.6 hours.

In another embodiment, the reaction according to Step C2 is carried outin THF with about 1.1 equivalents of a compound of formula Ar²—NHR₄ anda base, such as sodium bicarbonate (about 3 eq.), each relative to theCompound of Formula 16 (present at an initial concentration of about0.3M). The reaction mixture is kept at a temperature of about 0° C. forabout 5 min with stirring, warmed to about 25° C. over about 30 min,then heated to about 65° C. and kept at that temperature for about 1 hto provide an isonicotinamide Compound of Formula 18 a-l, which, afterthe THF is removed, e.g., under reduced pressure, can be used withoutfurther purification or, if desired, can be purified. For example, theCompound of Formula 18 a-l can be suspended in ethyl acetate and washedwith aqueous 3N HCl such that separate aqueous and organic layers form.The layers can be separated and the aqueous layer extracted with ethylacetate as required. The organic layer can be combined with thepost-extraction ethyl acetate aliquot(s), the combination dried, e.g.,with Na₂SO₄, and the solvent removed, e.g., under reduced pressure, toprovide a purified Compound of Formula 18 a-l. A Compound of Formula 18a-l is useful, e.g., as an intermediate for the synthesis of aCyclo(hetero)alkenyl Compound.

In Step C3 of Scheme C, the isonicotinamide Compound of Formula 18 a-lis reacted with an alkylating reagent of the formula Z—CH₂—R_(z), whereZ is Cl, Br or I, and R_(z) is —H; —(C₁-C₆)alkyl; —(C₃-C₈)cycloalkyl or-(3- to 7-membered)heterocyclo, each of which is optionally substitutedwith one or more R₅ groups; or -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to10-membered)heteroaryl, each of which is optionally substituted with oneor more R₆ groups; where R₅ and R₆ are defined above in connection withthe Cyclo(hetero)alkenyl Compounds of Formula (I). In one embodiment,the present invention relates to a method for making aCyclo(hetero)alkenyl Compound comprising allowing an isonicotinamideCompound of Formula 18 a-l to react with an alkylating reagent of theformula Z—CH₂—R_(z). In another embodiment, R_(z) is —H; —(C₁-C₆)alkyl;or -phenyl, which is optionally substituted with one or more R₆ groups.In another embodiment, R_(z) is —H, —(C₁-C₄)alkyl, or -phenyl which isunsubstituted. In another embodiment, R_(z) is -phenyl which isunsubstituted. Exemplary alkylating reagents include methyl iodide,methyl bromide, ethyl iodide, ethyl bromide, benzyl bromide, benzyliodide, benzyl chloride, 4-methoxybenzyl bromide, and 4-methoxybenzyliodide. In another embodiment, the alkylating reagent is a benzylatingreagent, i.e., comprises a benzyl group. Exemplary benzylating reagentsinclude benzyl bromide, benzyl iodide, benzyl chloride, 4-methoxybenzylbromide, 4-methoxybenzyl iodide, 4-methoxybenzyl chloride, or a mixturethereof. In another embodiment, the benzylating reagent is benzylbromide, benzyl iodide, benzyl chloride or a mixture thereof. In anotherembodiment, the benzylating reagent is benzyl bromide. In anotherembodiment, the benzylating reagent is benzyl iodide. In anotherembodiment, the benzylating reagent is benzyl chloride. In anotherembodiment, sodium iodide, potassium iodide, tetrabutylammonium iodide,or combinations thereof is present with an alkylating reagent comprisingchlorine.

In certain embodiments, the alkylating reagent is present in thereaction in Step C3 at an initial concentration within the range of fromabout 0.05M to about 2M, or at an initial concentration within the rangeof from about 0.1M to about 2M. In a specific embodiment, the Compoundof Formula 18 a-l is present in the reaction at an initial concentrationof about 0.35M.

In certain embodiments, the Compound of Formula 18 a-l is present in thereaction in Step C3 at an initial concentration within the range of fromabout 0.05M to about 5M, or at an initial concentration within the rangeof from about 0.1M to about 2M. In a specific embodiment, the Compoundof Formula 18 a-l is present in the reaction at an initial concentrationof about 0.24M.

In certain embodiments, the reaction Step C3 is carried out at atemperature within the range of from about 60° C. to about the boilingpoint of the solvent; at a temperature within the range of from about65° C. to about 100° C.; or at a temperature within the range of fromabout 75° C. to about 85° C.

In certain embodiments, the reaction in Step C3 is carried out in anonpolar solvent, e.g., hexane, heptane, benzene, diethyl ether, THF,DCM, DCE, chloroform, carbon tetrachloride and combinations thereof. Inone embodiment, the nonpolar solvent is THF, DMF or combinationsthereof. In another embodiment, the nonpolar solvent is a mixture of THFand DMF. In another embodiment, the mixture of THF:DMF is from about 8:1to about 1:1, or from about 5:1 to about 1:1 by volume. In anotherembodiment, the mixture of THF:DMF is about 4:1 by volume.

In certain embodiments, the Compound of Formula 18 a-l is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with thealkylating reagent. For example, the hydrochloride salt of the Compoundof Formula 18 a-l is dissolved in a suitable organic solvent, such asbut not limited to chloroform, to provide a solution that is extractedwith, e.g., a saturated aqueous solution of Na₂CO₃. The organic layer isrecovered and the aqueous layer back-extracted with an additional volumeof the organic solvent. The organic solvent layers are combined,extracted with water, dried, e.g., over anhydrous sodium sulfate, andthen the liquid is removed, such as by evaporation under reducedpressure, e.g., with a rotary evaporator, to provide the Compound ofFormula 18 a-l as the free amine.

The reaction in Step C3 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step C3 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step C3 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step C3 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step C3 is carried out under an argonatmosphere.

Progress of the reaction in Step C3 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step C3 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a1-alkylated-isonicotinamide Compound of Formula 19 a-l, to startingmaterial, the Compound of Formula 18 a-l, remains essentially constant.Typically, a time sufficient for the reaction in Step C3 is within therange of from about 1 hour to about 48 hours, from about 3 hours toabout 48 hours, or from about 10 hours to about 36 hours. In a specificembodiment, the reaction according to Step C3 is carried out for about24 hours.

In another embodiment, the reaction according to Step C3 is carried outin 4:1 THF:DMF by volume with the Compound of Formula 18 a-l present atan initial concentration of about 0.24M, with about a 0.35M initialconcentration of benzyl bromide, at a temperature of about 80° C., andfor a period of about 24 hours under reflux. Thereafter, the1-alkylated-isonicotinamide Compound of Formula 19 a-l is recoveredusing methods known to those skilled in the art. For example, thereaction mixture can be cooled to about 25° C. and the resulting solidcan be filtered off. A mjority of the THF can be removed from thefiltrate, e.g., under reduced pressure. Diethyl ether can be added tocause a precipitate to form from the DMF-enriched solution. Theresulting solid can be filtered off and the solids can be combined anddried to provide the 1-alkylated-isonicotinamide Compound of Formula 19a-l. A Compound of Formula 19 a-l is useful, e.g., as an intermediatefor the synthesis of a Cyclo(hetero)alkenyl Compound.

In Step C4 of Scheme C, the 1-alkylated-isonicotinamide Compound ofFormula 19 a-l is reacted with a hydrogenation agent, e.g., NaBH₄ orLiBH₄. In one embodiment, the present invention relates to a method formaking a Cyclo(hetero)alkenyl Compound comprising allowing a1-alkylated-isonicotinamide Compound of Formula 19 a-l to react with ahydrogenation agent. In another embodiment, the hydrogenation agent isNaBH₄, LiBH₄ or a mixture thereof. In another embodiment, thehydrogenation agent is NaBH₄. Hydrogenation agents are commerciallyavailable from, e.g., Aldrich Chemical Co., or can be prepared bymethods known to those skilled in the art.

In certain embodiments, the reaction in Step C4 is carried out with aninitial amount of hydrogenation agent within the range of from about 1to about 10 equivalents, or within the range of from about 1 to about 6equivalents, on a molar basis, relative to the Compound of Formula 19a-l. In another embodiment, this reaction is carried out with about 3.2equivalents, on a molar basis, of hydrogenation agent, relative to theCompound of Formula 19 a-l.

In certain embodiments, the Compound of Formula 19 a-l is present in thereaction in Step C4 at an initial concentration within the range of fromabout 0.01M to about 5M, or at an initial concentration within the rangeof from about 0.05M to about 2M. In a specific embodiment, the Compoundof Formula 19 a-l is present in the reaction at an initial concentrationof about 0.18M.

In certain embodiments, the reaction in Step C4 is carried out at atemperature within the range of from about −10° C. to about 50° C.; at atemperature within the range of from about −10° C. to about 40° C.; orat a temperature within the range of from about 0° C. to about 30° C.

In certain embodiments, the reaction in Step C4 is carried out in apolar protic nonaqueous solvent, such as an alcohol, e.g., methanol,ethanol, a dialkylamide, e.g., dimethyl formamide dimethyl formamide,methyl ethyl formamide, or combinations thereof. In one embodiment, thepolar protic nonaqueous solvent is an alcohol, a dialkylamide orcombinations thereof. In another embodiment, the polar protic nonaqueoussolvent is methanol, ethanol, isopropanol or combinations thereof. Inanother embodiment, the polar protic nonaqueous solvent is methanol. Inanother embodiment, the polar protic nonaqueous solvent is dimethylformamide, dimethyl formamide, methyl ethyl formamide or combinationsthereof. In another embodiment, the polar protic nonaqueous solvent isdimethyl formamide.

The reaction in Step C4 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step C4 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step C4 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step C4 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step C4 is carried out under an argonatmosphere.

Progress of the reaction in Step C4 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step C4 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a1-alkylated-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide Compoundof Formula 20 a-l, to starting material, the Compound of Formula 19 a-l,remains essentially constant. Typically, a time sufficient for thereaction in Step C4 is within the range of from about 5 minutes to about10 hours, from about 5 minutes to about 5 hours, or from about 15minutes to about 5 hours. In a specific embodiment, the reactionaccording to Step C4 is carried out for about 3.5 hours.

In another embodiment, the reaction according to Step C4 is carried outat about 0° C. in an alcohol with about 3.2 equivalents, on a molarbasis, of a hydrogenation agent, relative to the Compound of Formula 19a-l, added portion-wise over a period of about 30 min. Thereafter, thereaction mixture can be stirred for about 1 h at about 0° C. and warmedto about 25° C. over about a 2 hour period to provide a1-alkylated-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide Compoundof Formula 20 a-l, which, after the alcohol is removed, e.g., underreduced pressure, can be used without further purification or, ifdesired, can be purified. For example, the Compound of Formula 20 a-lcan be diluted with brine and ethyl acetate such that separate aqueousand organic layers form. The layers can be separated and the aqueouslayer washed with ethyl acetate as required. The organic layer can becombined with the post-washing ethyl acetate aliquot(s), the combinationdried, e.g., with Na₂SO₄, and the solvent removed, e.g., under reducedpressure, to provide purified Compound of Formula 20 a-l which can beused without additional purification or, if desired, can be furtherpurified. For example, the purified Compound of Formula 20 a-l can bedissolved in DCM and precipitated by adding hexane to the DCM solution.The resulting solid can be filtered off and dried to provide furtherpurified Compound of Formula 20 a-l. A Compound of Formula 20 a-l isuseful, e.g., as an intermediate for the synthesis of aCyclo(hetero)alkenyl Compound.

In Step C5 of Scheme C, the1-alkylated-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide Compoundof Formula 20 a-l is reacted with a dealkylating reagent, e.g.,α-chloroethylchloroformate. In one embodiment, the present inventionrelates to a method for making a Cyclo(hetero)alkenyl Compoundcomprising allowing a1-alkylated-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide Compoundof Formula 20 a-l to react with a dealkylating reagent. In anotherembodiment, the dealkylating reagent is a-chloroethylchloroformate,2,2,2-trichloroethylchloroformate or a mixture thereof. In anotherembodiment, the dealkylating reagent is a-chloroethylchloroformate. Inanother embodiment, the dealkylating reagent is2,2,2-trichloroethylchloroformate. Dealkylating reagents arecommercially available from, e.g., Aldrich Chemical Co., or can beprepared by methods known to those skilled in the art.

In certain embodiments, the dealkylating reagent is present in thereaction in Step C5 at an initial concentration within the range of fromabout 0.05M to about 4M, or at an initial concentration within the rangeof from about 0.06M to about 4M. In a specific embodiment, thedealkylating reagent is present in the reaction at an initialconcentration of about 0.32M.

In certain embodiments, the Compound of Formula 20 a-l is present in thereaction in Step C5 at an initial concentration within the range of fromabout 0.01M to about 5M, or at an initial concentration within the rangeof from about 0.05M to about 2M. In a specific embodiment, the Compoundof Formula 20 a-l is present in the reaction at an initial concentrationof about 0.17M.

In certain embodiments, the reaction in Step C5 is carried out at atemperature within the range of from about 0° C. to about the boilingpoint of the solvent; at a temperature within the range of from about 0°C. to about 100° C.; or at a temperature within the range of from about0° C. to about 90° C.

In certain embodiments, the reaction in Step C5 is carried out in anonpolar solvent, e.g., hexane, heptane, benzene, diethyl ether, THF,DCM, DCE, chloroform, carbon tetrachloride and combinations thereof. Inone embodiment, the nonpolar solvent is DCE, THF or combinationsthereof. In another embodiment, the nonpolar solvent is DCE. In anotherembodiment, the nonpolar solvent is THF.

In certain embodiments, the Compound of Formula 20 a-l is provided as asalt, e.g., the hydrochloride salt, which can be converted to the freeamine, using procedures known in the art, prior to reaction with thedealkylating reagent. For example, the hydrochloride salt of theCompound of Formula 20 a-l is dissolved in a suitable organic solvent,such as but not limited to chloroform, to provide a solution that isextracted with, e.g., a saturated aqueous solution of Na₂CO₃. Theorganic layer is recovered and the aqueous layer back-extracted with anadditional volume of the organic solvent. The organic solvent layers arecombined, extracted with water, dried, e.g., over anhydrous sodiumsulfate, and then the liquid is removed, such as by evaporation underreduced pressure, e.g., with a rotary evaporator, to provide theCompound of Formula 20 a-l as the free amine.

The reaction in Step C5 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step C5 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step C5 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step C5 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step C5 is carried out under an argonatmosphere.

Progress of the reaction in Step C5 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step C5 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, a1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide Compound of Formula21 a-l, to starting material, the Compound of Formula 20 a-l, remainsessentially constant. Typically, a time sufficient for the reaction inStep C5 is within the range of from about 0.3 hours to about 48 hours,from about 0.5 hours to about 48 hours, or from about 0.5 hours to about5 hours. In a specific embodiment, the reaction according to Step C5 iscarried out for about 4.75 hours.

In another embodiment, the reaction according to Step C5 is carried outin DCE with the Compound of Formula 20 a-l present at an initialconcentration of about 0.17M, with about a 0.32M initial concentrationof α-chloroethylchloroformate (after adding drop-wise over a 15 minuteperiod) at a temperature of about 0° C. The reaction mixture can bewarmed to about 25° C. over a period of about 30 min then heated toabout 83° C. for about 4 hours at that temperature to provide a1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide Compound of Formula21 a-l, which, after the solvent and unreactedα-chloroethylchloroformate are removed, e.g., under reduced pressure,can be used without further purification or, if desired, can bepurified. For example, the Compound of Formula 21 a-l can be dissolvedin methanol, refluxed for about 3 hours at a temperature of about 65°C., and the methanol removed, e.g., under reduced pressure, to providepurified Compound of Formula 21 a-l which can be used without additionalpurification or, if desired, can be further purified. For example, thepurified Compound of Formula 21 a-l can be dissolved in DCM andprecipitated by adding diethyl ether to the DCM solution. The resultingsolid can be filtered off and dried to provide further purified Compoundof Formula 21 a-l. A Compound of Formula 21 a-l is useful, e.g., as anintermediate for the synthesis of a Cyclo(hetero)alkenyl Compound.

In Step C6 of Scheme C, the 1,2,3,6-tetrahydro-pyridine-4-carboxylicacid amide Compound of Formula 21 a-l is reacted with a compound offormula Ar¹—Z, where Z is Cl, Br or I. In one embodiment, the presentinvention relates to a method for making a Cyclo(hetero)alkenyl Compoundcomprising allowing a 1,2,3,6-tetrahydro-pyridine-4-carboxylic acidamide Compound of Formula 21 a-l to react with a compound of formulaAr¹—Z. In another embodiment, the compound of formula Ar¹—Z is2-chloro-3-nitropyridine. In another embodiment, the compound of formulaAr¹—Z is 2,3-dichlnropyridine. In another embodiment, compound offormula Ar¹—Z is 2-chloro-3-fluoropyridine.

In certain embodiments, the compound of formula Ar¹—Z is present in thereaction in Step C6 at an initial concentration within the range of fromabout 0.01M to about 5M, or at an initial concentration within the rangeof from about 0.05M to about 3M. In a specific embodiment, the compoundof formula Ar¹—Z is present in the reaction at an initial concentrationof about 0.064M.

In certain embodiments, the Compound of Formula 21 a-l is present in thereaction in Step C6 at an initial concentration within the range of fromabout 0.01M to about 5M, or at an initial concentration within the rangeof from about 0.05M to about 3M. In a specific embodiment, the Compoundof Formula 21 a-l is present in the reaction at an initial concentrationof about 0.068M.

In certain embodiments, a trialkylamine, such as triethylamine,trimethylamine, methyl diethylamine or diisopropyl ethylamine, ispresent in the reaction in Step C6 at an initial concentration withinthe range of from about 0.01M to about 5M, or at an initialconcentration within the range of from about 0.05M to about 3M. In aspecific embodiment, the trialkylamine is present in the reaction at aninitial concentration of about 0.27M. In one embodiment, thetrialkylamine is triethylamine, trimethylamine, methyl diethylamine,diisopropyl ethylamine or combinations thereof. In another embodiment,the trialkylamine is triethylamine.

In certain embodiments, the reaction in Step C6 is carried out at atemperature within the range of from about 15° C. to about 140° C.; at atemperature within the range of from about 25° C. to about 140° C.; orat a temperature within the range of from about 15° C. to about 30° C.

In certain embodiments, the reaction in Step C6 is carried out in asolvent, e.g., hexane, heptane, benzene, diethyl ether, TRF, DCM, DCE,chloroform, carbon tetrachloride, DMF, DMSO, and combinations thereof.In one embodiment, the nonpolar solvent is DCE, THF or combinationsthereof. In another embodiment, the nonpolar solvent is DCE.

The reaction in Step C6 can be carried out at reduced pressure,atmospheric pressure or elevated pressure, i.e., greater thanatmospheric pressure. In one embodiment, the reaction is carried out atatmospheric pressure. In certain embodiments, the reaction in Step C6 iscarried out in an air atmosphere. In certain embodiments, the reactionin Step C6 is carried out in an inert atmosphere. In one non-limitingaspect of this embodiment, the reaction in Step C6 is carried out undera nitrogen atmosphere. In another non-limiting aspect of thisembodiment, the reaction in Step C6 is carried out under an argonatmosphere.

Progress of the reaction in Step C6 can be monitored using conventionalanalytical techniques, including but not limited to IR, LC, MS, LCMS,TLC, HPLC, GC, GLC and/or NMR. The reaction according to Step C6 iscarried out, in one embodiment, until a starting material is consumedor, in another embodiment, until the ratio of product, theCyclo(hetero)alkenyl Compound, to starting material, the Compound ofFormula 21 a-l, remains essentially constant. Typically, a timesufficient for the reaction in Step C6 is within the range of from about0.5 hours to about 48 hours, from about 0.5 hours to about 36 hours, orfrom about 3 hours to about 24 hours. In a specific embodiment, thereaction according to Step C6 is carried out for about 12 hours.

In another embodiment, the reaction according to Step C6 is carried outin DCE with about 0.064M of a compound of formula Ar¹—Z, about 0.068M ofa Compound of Formula 21 a-l, and about 0.27M of a trialkylamine, suchas triethylamine, trimethylamine, methyl diethylamine or diisopropylethylamine. The reaction mixture is kept at a temperature within therange of from about 20° C. to about 30° C. for a period of about 12hours with stirring. Thereafter, the mixture can be poured into aqueoussodium bicarbonate and DCM such that separate aqueous and organic layersform. The organic layer is separated from the aqueous layer. The organiclayer is dried, e.g., with Na₂SO₄, and the solvent is removed, e.g.,under reduced pressure, to provide a residue that can be used withoutfurther purification or, if desired, can be purified to provide aCyclo(hetero)alkenyl Compound where V is N. For example, the residue canbe dissolved in DCM and precipitated by adding hexane to the DCMsolution. The resulting solid can be filtered off and dried to provide apurified Cyclo(hetero)alkenyl Compound where V is N. As discussed above,if a mixture of Cyclo(hetero)alkenyl Compounds is obtained where m=1,the mixture can be separated by conventional methods, for example,column chromatography.

The Compound of Formula (I) where X is S (i.e., the Compound of Formula(II′)) can be made by, e.g., reacting a Compound of Formula (II) (i.e.,where X is O) with Lawesson's reagent as described in connection withScheme A.

Thus, in another embodiment, a method for preparing aCyclo(hetero)alkenyl Compound comprises allowing a1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide compound to reactwith a compound of formula Ar¹—Z to provide a Cyclo(hetero)alkenylCompound; where Z is Cl, Br or I.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing a1-alkylated-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide compoundto react with a dealkylating reagent to provide a1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amide compound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing a 1-alkylated-isonicotinamide compound toreact with a hydrogenation agent to provide a1-alkylated-1,2,3,6-tetrahydro-pyridine-4-carboxylic acid amidecompound.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises allowing an isonicotinamide compound to react with analkylating reagent to provide a 1-alkylated-isonicotinamide compound.

In another embodiment, in method for preparing a Cyclo(hetero)alkenylCompound, the alkylating reagent is a benzylating reagent selected frombenzyl bromide, benzyl iodide, benzyl chloride or a mixture thereof.

In another embodiment, a method for preparing a Cyclo(hetero)alkenylCompound comprises forming the isonicotinamide compound by allowing anisonicotinolyl chloride compound to react with a compound of formulaAr²—NHR₄;

where R₄ is —H or —(C₁-C₆)alkyl; and

Ar² is

where Y₁ and Y₂ are —CH₂— and —CH₂—, —O— and —O—, —NH— and —NH—, —S— and—S—, —CH₂— and —O—, —CH₂— and —NH—, —CH₂— and —S—, —O— and —CH₂—, —NH—and —CH₂—, —S— and —CH₂—, —O— and —NH—, —NH— and —O—, —S— and —NH—, or—NH— and —S— respectively;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each R₈ is independently —(C₁-C₁₀)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇, —R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇,—R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂,—(C₁-C₁₀)alkyl, or -(3- to 7-membered)heterocycle;

each R₉ is independently —H, -halo or —(C₁-C₆)alkyl;

each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR_(S), —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇;

each halo is independently —F, —Cl, —Br, or —I;

q is an integer ranging from 0 to 6;

r is an integer ranging from 0 to 5; and

s is an integer ranging from 0 to 4.

In another embodiment, the present invention relates to a compound offormula 18 a-l

or a pharmaceutically acceptable salt thereof, where:

Ar² is

Y₁ and Y₂ are —CH₂— and —CH₂—, —O— and —O—, —NH— and —NH—, —S— and —S—,—CH₂— and —O—, —CH₂— and —NH—, —CH₂— and —S—, —O— and —CH₂—, —NH— and—CH₂—, —S— and —CH₂—, —O— and —NH—, —NH— and —O—, —S— and —NH—, or —NH—and —S— respectively;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

R₄ is —H or —(C₁-C₆)alkyl;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each R₈ is independently —(C₁-C₁₀)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇, —R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇,—R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂,—(C₁-C₁₀)alkyl, or -(3- to 7-membered)heterocycle;

each R₉ is independently —H, -halo or —(C₁-C₆)alkyl;

each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇;

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

q is an integer ranging from 0 to 6;

r is an integer ranging from 0 to 5; and

s is an integer ranging from 0 to 4.

In another embodiment, the present invention relates to a compound offormula 19 a-l

or a pharmaceutically acceptable salt thereof, where:

Ar² is

Y₁ and Y₂ are —CH₂— and —CH₂—, —O— and —O—, —NH— and —NH—, —S— and —S—,—CH₂— and —O—, —CH₂— and —NH—, —CH₂— and —S—, —O— and —CH₂—, —NH— and—CH₂—, —S— and —CH₂—, —O— and —NH—, —NH— and —O—, —S— and —NH—, or —NH—and —S— respectively;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

R₄ is —H or —(C₁-C₆)alkyl;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR_(S), —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each R₈ is independently —(C₁-C₁₀)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇, —R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇,—R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂,—(C₁-C₁₀)alkyl, or -(3- to 7-membered)heterocycle;

each R₉ is independently —H, -halo or —(C₁-C₆)alkyl;

each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇;

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

q is an integer ranging from 0 to 6;

r is an integer ranging from 0 to 5;

s is an integer ranging from 0 to 4;

R_(z) is -phenyl which is optionally substituted with one or more R₆groups, —H or —(C₁-C₆)alkyl; and

Z is Cl, Br or I.

In another embodiment, the present invention relates to a compound offormula 20 a-l

or a pharmaceutically acceptable salt thereof, where:

Ar² is

Y₁ and Y₂ are —CH₂— and —CH₂—, —O— and —O—, —NH— and —NH—, —S— and —S—,—CH₂— and —O—, —CH₂— and —NH—, —CH₂— and —S—, —O— and —CH₂—, —NH— and—CH₂—, —S— and —CH₂—, —O— and —NH—, —NH— and —O—, —S— and —NH—, or —NH—and —S— respectively;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

R₄ is —H or —(C₁-C₆)alkyl;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each R₈ is independently —(C₁-C₁₀)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇, —R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇,—R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂,—(C₁-C₁₀)alkyl, or -(3- to 7-membered)heterocycle;

each R₉ is independently —H, -halo or —(C₁-C₆)alkyl;

each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇;

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

q is an integer ranging from 0 to 6;

r is an integer ranging from 0 to 5;

s is an integer ranging from 0 to 4; and

R_(z) is -phenyl which is optionally substituted with one or more R₆groups, —H or —(C₁-C₆)alkyl.

In another embodiment, the present invention relates to a compound offormula 21 a-l

or a pharmaceutically acceptable salt thereof, where:

Ar² is

Y₁ and Y₂ are —CH₂— and —CH₂—, —O— and —O—, —NH— and —NH—, —S— and —S—,—CH₂— and —O—, —CH₂— and —NH—, —CH₂— and —S—, —O— and —CH₂—, —NH— and—CH₂—, —S— and —CH₂—, —O— and —NH—, —NH— and —O—, —S— and —NH—, or —NH—and —S— respectively;

each R₃ is independently:

-   -   (a) -halo, —CN, —OH, —NO₂, or —NH₂,    -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,        —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,        —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,        —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to        7-membered)heterocycle, or -(7- to        10-membered)bicycloheterocycle, each of which is unsubstituted        or substituted with one or more R₅ groups, or    -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)        heteroaryl, each of which is unsubstituted or substituted with        one or more R₆ groups;

R₄ is —H or —(C₁-C₆)alkyl;

each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR_(S), —S(O)R₇, or —S(O)₂R₇;

each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;

each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3-to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo);

each R₈ is independently —(C₁-C₁₀)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇, —R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇,—R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂,—CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃,—OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂,—(C₁-C₁₀)alkyl, or -(3- to 7-membered)heterocycle;

each R₉ is independently —H, -halo or —(C₁-C₆)alkyl;

each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,—COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇;

each halo is independently —F, —Cl, —Br, or —I;

m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or6-position of the cyclo(hetero)alkenyl ring;

q is an integer ranging from 0 to 6;

r is an integer ranging from 0 to 5; and

s is an integer ranging from 0 to 4.

4.3.2 Methods for Making the Cyclo(Hetero)Alkenyl Compounds where V isCh

In another embodiment, the present invention relates to methods formaking the Cyclo(hetero)alkenyl Compounds where V is CH by the followingnon-limiting illustrative method shown below in Scheme D.

where R₁, R₂, R₃, R₄, Ar¹, Ar², m, n and p are defined above.

A Compound of Formula 1 a-h is reacted with butyl lithium in diethylether/THF and then with a Compound of Formula 7 according to theprocedure described in J. Med. Chem. 32(2):351-7 (1989) to provide aCompound of Formula 8 a-h. In one embodiment, the present inventionrelates to a method for making a Cyclo(hetero)alkenyl Compoundcomprising allowing a Compound of Formula 1 a-h to react with butyllithium and then with a Compound of Formula 7. A Compound of Formula 8a-h is useful, e.g., as an intermediate for the synthesis of aCyclo(hetero)alkenyl Compound.

The Compound of Formula 8 a-h is then reacted with a Lewis acid, e.g.,SOCl₂/pyridine, hydrogenated using a Pd catalyst in ethyl acetate, andreacted with trifluoroacetic acid in water according to the proceduredescribed in J. Med. Chem. 32(2):351-7 (1989) to provide a Compound ofFormula 9 a-h. In one embodiment, the present invention relates to amethod for making a Cyclo(hetero)alkenyl Compound comprising allowing aCompound of Formula 8 a-h to react with a Lewis acid, then hydrogenatingthe product, and allowing the hydrogenated product to react withtrifluoroacetic acid. A Compound of Formula 9 a-h is useful, e.g., as anintermediate for the synthesis of a Cyclo(hetero)alkenyl Compound.

The Compound of Formula 9 a-h is then reacted with (CF₃SO₂)₂O in thepresence of methyl-di-(tert-butyl)-pyridine in DCM according to theprocedure described in J. Org. Chem. 54(12):2886-9 (1989) or OrganicSyntheses 68:116-29 (1980) to provide a Compound of Formula 10 a-h. Inone embodiment, the present invention relates to a method for making aCyclo(hetero)alkenyl Compound comprising allowing a Compound of Formula9 a-h to react with (CF₃SO₂)₂O. In another embodiment, this reaction isin the presence of methyl-di-(tert-butyl)-pyridine. A Compound ofFormula 10 a-h is useful, e.g., as an intermediate for the synthesis ofa Cyclo(hetero)alkenyl Compound.

The Compound of Formula 10 a-h is then reacted with an amine of formulaAr²⁻NHR₄ in the presence of palladium pentadione, triphenylphosphine,and lithium chloride in THF under an atmosphere of carbon monoxideaccording to the procedure described in Tetrahedron Letters 33(9):1181-4(1992) to provide the Cyclo(hetero)alkenyl Compound where V is CH. Inone embodiment, the present invention relates to a method for making aCyclo(hetero)alkenyl Compound comprising allowing a Compound of Formula10 a-h to react with an amine of formula Ar²⁻NHR₄. In anotherembodiment, this reaction is in the presence of palladium pentadione,triphenylphosphine, and lithium chloride. In another embodiment, thisreaction is under an atmosphere of carbon monoxide.

Compounds of formula 7 are commercially available or can be prepared bymethods known to those skilled in the art.

Where m=1, a mixture of Cyclo(hetero)alkenyl Compounds is generallyobtained. The mixture can be separated by conventional methods, forexample, column chromatography.

The Compound of Formula (I) where X is S (i.e., the Compound of Formula(III′)) can be made by, e.g., reacting a Compound of Formula (III)(i.e., where X is O) with Lawesson's reagent as described in connectionwith Scheme A. This reaction is illustrated below:

Certain Cyclo(hetero)alkenyl Compounds can have asymmetric centers andtherefore exist in different enantiomeric and diastereomeric forms. ACyclo(hetero)alkenyl Compound can be in the form of an optical isomer ora diastereomer. Accordingly, the invention encompassesCyclo(hetero)alkenyl Compounds and their uses as described herein in theform of their optical isomers, diasteriomers and mixtures thereof,including a racemic mixture. Optical isomers of the Cyclo(hetero)alkenylCompounds can be obtained by known techniques such as chiralchromatography or formation of diastereomeric salts from an opticallyactive acid or base.

In addition, one or more hydrogen, carbon or other atoms of aCyclo(hetero)alkenyl Compound can be replaced by an isotope of thehydrogen, carbon or other atoms. Such compounds, which are encompassedby the present invention, are useful as research and diagnostic tools inmetabolism pharmacokinetic studies and in binding assays.

4.4 Therapeutic Uses of the Cyclo(Hetero)Alkenyl Compounds

In accordance with the invention, the Cyclo(hetero)alkenyl Compounds areadministered to an animal in need of treatment or prevention of aCondition.

In one embodiment, an effective amount of a Cyclo(hetero)alkenylCompound can be used to treat or prevent any condition treatable orpreventable by inhibiting VR1. Examples of conditions that are treatableor preventable by inhibiting VR1 include, but are not limited to, pain,UI, an ulcer, IBD, and IBS.

In another embodiment, an effective amount of a Cyclo(hetero)alkenylCompound can be used to treat or prevent any condition treatable orpreventable by inhibiting mGluR5. Examples of conditions that aretreatable or preventable by inhibiting mGluR5 include, but are notlimited to, pain, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, a pruritic condition, and psychosis.

In another embodiment, an effective amount of a Cyclo(hetero)alkenylCompound can be used to treat or prevent any condition treatable orpreventable by inhibiting mGluR1. Examples of conditions that aretreatable or preventable by inhibiting mGluR1 include, but are notlimited to, pain, UI, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, and depression.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent acuteor chronic pain. Examples of pain treatable or preventable using theCyclo(hetero)alkenyl Compounds include, but are not limited to, cancerpain, labor pain, myocardial infarction pain, pancreatic pain, colicpain, post-operative pain, headache pain, muscle pain, arthritic pain,and pain associated with a periodontal disease, including gingivitis andperiodontitis.

The Cyclo(hetero)alkenyl Compounds can also be used for treating orpreventing pain associated with inflammation or with an inflammatorydisease in an animal. Such pain can arise where there is an inflammationof the body tissue which can be a local inflammatory response and/or asystemic inflammation. For example, the Cyclo(hetero)alkenyl Compoundscan be used to treat or prevent pain associated with inflammatorydiseases including, but not limited to: organ transplant rejection;reoxygenation injury resulting from organ transplantation (see Grupp etal., J. Mol. Cell Cardiol. 31:297-303 (1999)) including, but not limitedto, transplantation of the heart, lung, liver, or kidney; chronicinflammatory diseases of the joints, including arthritis, rheumatoidarthritis, osteoarthritis and bone diseases associated with increasedbone resorption; inflammatory lung diseases, such as asthma, adultrespiratory distress syndrome, and chronic obstructive airway disease;inflammatory diseases of the eye, including corneal dystrophy, trachoma.onchocerciasis, uveitis, sympathetic ophthalmitis and endophthalmitis;chronic inflammatory diseases of the gum, including gingivitis andperiodontitis; tuberculosis; leprosy; inflammatory diseases of thekidney, including uremic complications, glomerulonephritis andnephrosis; inflammatory diseases of the skin, includingsclerodermatitis, psoriasis and eczema; inflammatory diseases of thecentral nervous system, including chronic demyelinating diseases of thenervous system, multiple sclerosis, AIDS-related neurodegeneration andAlzheimer s disease, infectious meningitis, encephalomyelitis,Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosisand viral or autoimmune encephalitis; autoimmune diseases, includingType I and Type II diabetes mellitus; diabetic complications, including,but not limited to, diabetic cataract, glaucoma, retinopathy,nephropathy (such as microaluminuria and progressive diabeticnephropathy), polyneuropathy, mononeuropathies, autonomic neuropathy,gangrene of the feet, atherosclerotic coronary arterial disease,peripheral arterial disease, nonketotic hyperglycemic-hyperosmolar coma,foot ulcers, joint problems, and a skin or mucous membrane complication(such as an infection, a shin spot, a candidal infection or necrobiosislipoidica diabeticorum); immune-complex vasculitis, and systemic lupuserythematosus (SLE); inflammatory diseases of the heart, such ascardiomyopathy, ischemic heart disease hypercholesterolemia, andatherosclerosis; as well as various other diseases that can havesignificant inflammatory components, including preeclampsia, chronicliver failure, brain and spinal cord trauma, and cancer. TheCyclo(hetero)alkenyl Compounds can also be used for treating orpreventing pain associated with inflammatory disease that can, forexample, be a systemic inflammation of the body, exemplified bygram-positive or gram negative shock, hemorrhagic or anaphylactic shock,or shock induced by cancer chemotherapy in response to pro-inflammatorycytokines, e.g., shock associated with pro-inflammatory cytokines. Suchshock can be induced, e.g., by a chemotherapeutic agent that isadministered as a treatment for cancer.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent UI.Examples of UI treatable or preventable using the Cyclo(hetero)alkenylCompounds include, but are not limited to, urge incontinence, stressincontinence, overflow incontinence, neurogenic incontinence, and totalincontinence.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent anulcer. Examples of ulcers treatable or preventable using theCyclo(hetero)alkenyl Compounds include, but are not limited to, aduodenal ulcer, a gastric ulcer, a marginal ulcer, an esophageal ulcer,or a stress ulcer.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent IBD,including Crohn's disease and ulcerative colitis.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent IBS.Examples of IBS treatable or preventable using the Cyclo(hetero)alkenylCompounds include, but are not limited to, spastic-colon-type IBS andconstipation-predominant IBS.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent anaddictive disorder, including but not limited to, an eating disorder, animpulse-control disorder, an alcohol-related disorder, anicotine-related disorder, an amphetamine-related disorder, acannabis-related disorder, a cocaine-related disorder, anhallucinogen-related disorder, an inhalant-related disorders, and anopioid-related disorder, all of which are further sub-classified aslisted below.

Eating disorders include, but are not limited to, Bulimia Nervosa,Nonpurging Type; Bulimia Nervosa, Purging Type; Anorexia; and EatingDisorder not otherwise specified (NOS).

Impulse control disorders include, but are not limited to, IntermittentExplosive Disorder, Kleptomania, Pyromania, Pathological Gambling,Trichotillomania, and Impulse Control Disorder not otherwise specified(NOS).

Alcohol-related disorders include, but are not limited to,Alcohol-Induced Psychotic Disorder with delusions, Alcohol Abuse,Alcohol Intoxication, Alcohol Withdrawal, Alcohol Intoxication Delirium,Alcohol Withdrawal Delirium, Alcohol-Induced Persisting Dementia,Alcohol-Induced Persisting Amnestic Disorder, Alcohol Dependence,Alcohol-Induced Psychotic Disorder with hallucinations, Alcohol-InducedMood Disorder, Alcohol-Induced Anxiety Disorder, Alcohol-Induced SexualDysfunction, Alcohol-Induced Sleep Disorder, and Alcohol-RelatedDisorder not otherwise specified (NOS).

Nicotine-related disorders include, but are not limited to, NicotineDependence, Nicotine Withdrawal, and Nicotine-Related Disorder nototherwise specified (NOS).

Amphetamine-related disorders include, but are not limited to,Amphetamine Dependence, Amphetamine Abuse, Amphetamine Intoxication,Amphetamine Withdrawal, Amphetamine Intoxication Delirium,Amphetamine-Induced Psychotic Disorder with delusions,Amphetamine-Induced Psychotic Disorders with hallucinations,Amphetamine-Induced Mood Disorder, Amphetamine-Induced Anxiety Disorder,Amphetamine-Induced Sexual Dysfunction, Amphetamine-Induced SleepDisorder, Amphetamine Related Disorder not otherwise specified (NOS),Amphetamine Intoxication, and Amphetamine Withdrawal.

Cannabis-related disorders include, but are not limited to, CannabisDependence, Cannabis Abuse, Cannabis Intoxication, Cannabis IntoxicationDelirium, Cannabis-Induced Psychotic Disorder with delusions,Cannabis-Induced Psychotic Disorder with hallucinations,Cannabis-Induced Anxiety Disorder, Cannabis Related Disorder nototherwise specified (NOS), and Cannabis Intoxication.

Cocaine-related disorders include, but are not limited to, CocaineDependence, Cocaine Abuse, Cocaine Intoxication, Cocaine Withdrawal,Cocaine Intoxication Delirium, Cocaine-Induced Psychotic Disorder withdelusions, Cocaine-Induced Psychotic Disorders with hallucinations,Cocaine-Induced Mood Disorder, Cocaine-Induced Anxiety Disorder,Cocaine-Induced Sexual Dysfunction, Cocaine-Induced Sleep Disorder,Cocaine Related Disorder not otherwise specified (NOS), CocaineIntoxication, and Cocaine Withdrawal.

Hallucinogen-related disorders include, but are not limited to,Hallucinogen Dependence, Hallucinogen Abuse, Hallucinogen Intoxication,Hallucinogen Withdrawal, Hallucinogen Intoxication Delirium,Hallucinogen-Induced Psychotic Disorder with delusions,Hallucinogen-Induced Psychotic Disorders with hallucinations,Hallucinogen-Induced Mood Disorder, Hallucinogen-Induced AnxietyDisorder, Hallucinogen-Induced Sexual Dysfunction, Hallucinogen-InducedSleep Disorder, Hallucinogen Related Disorder not otherwise specified(NOS), Hallucinogen Intoxication, and Hallucinogen Persisting PerceptionDisorder (Flashbacks).

Inhalant-related disorders include, but are not limited to, InhalantDependence, Inhalant Abuse, Inhalant Intoxication, Inhalant IntoxicationDelirium, Inhalant-Induced Psychotic Disorder with delusions,Inhalant-Induced Psychotic Disorder with hallucinations,Inhalant-Induced Anxiety Disorder, Inhalant Related Disorder nototherwise specified (NOS), and Inhalant Intoxication.

Opioid-related disorders include, but are not limited to, OpioidDependence, Opioid Abuse, Opioid Intoxication, Opioid IntoxicationDelirium, Opioid-Induced Psychotic Disorder with delusions,Opioid-Induced Psychotic Disorder with hallucinations, Opioid-InducedAnxiety Disorder, Opioid Related Disorder not otherwise specified (NOS),Opioid Intoxication, and Opioid Withdrawal.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventParkinson's disease and parkinsonism and the symptoms associated withParkinson's disease and parkinsonism, including but not limited to,bradykinesia, muscular rigidity, resting tremor, and impairment ofpostural balance.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventgeneralized anxiety or severe anxiety and the symptoms associated withanxiety, including but not limited to, restlessness; tension;tachycardia; dyspnea; depression, including chronic “neurotic”depression; panic disorder; agoraphobia and other specific phobias;eating disorders; and personality disorders.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventepilepsy, including but not limited to, partial epilepsy, generalizedepilepsy, and the symptoms associated with epilepsy, including but notlimited to, simple partial seizures, jacksonian seizures, complexpartial (psychomotor) seizures, convulsive seizures (grand mal ortonic-clonic seizures), petit mal (absence) seizures, and statusepilepticus.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventstrokes, including but not limited to, ischemic strokes and hemorrhagicstrokes.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent aseizure, including but not limited to, infantile spasms, febrileseizures, and epileptic seizures.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent apruritic condition, including but not limited to, pruritus caused by dryskin, scabies, dermatitis, herpetiformis, atopic dermatitis, pruritusvulvae et ani, miliaria, insect bites, pediculosis, contact dermatitis,drug reactions, urticaria, urticarial eruptions of pregnancy, psoriasis,lichen planus, lichen simplex chronicus, exfoliative dermatitis,folliculitis, bullous pemphigoid, or fiberglass dermatitis.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventpsychosis, including but not limited to, schizophrenia, includingparanoid schizophrenia, hebephrenic or disorganized schizophrenia,catatonic schizophrenia, undifferentiated schizophrenia, negative ordeficit subtype schizophrenia, and non-deficit schizophrenia; adelusional disorder, including erotomanic subtype delusional disorder,grandiose subtype delusional disorder, jealous subtype delusionaldisorder, persecutory subtype delusional disorder, and somatic subtypedelusional disorder; and brief psychosis.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent acognitive disorder, including but not limited to, delirium and dementiasuch as multi-infarct dementia, dementia pugilistica, dementia caused byAIDS, and dementia caused by Alzheimer's disease.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent amemory deficiency, including but not limited to, dissociative amnesiaand dissociative fugue.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventrestricted brain function, including but not limited to, that caused bysurgery or an organ transplant, restricted blood supply to the brain, aspinal cord injury, a head injury, hypoxia, cardiac arrest, orhypoglycemia.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventHuntington's chorea.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent ALS.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventretinopathy, including but not limited to, arteriosclerotic retinopathy,diabetic arteriosclerotic retinopathy, hypertensive retinopathy,non-proliferative retinopathy, and proliferative retinopathy.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent amuscle spasm.

The Cyclo(hetero)alkenyl Compounds can be used to treat or prevent amigraine.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventvomiting, including but not limited to, nausea vomiting, dry vomiting(retching), and regurgitation.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventdyskinesia, including but not limited to, tardive dyskinesia and biliarydyskinesia.

The Cyclo(hetero)alkenyl Compounds can be used to treat or preventdepression, including but not limited to, major depression and bipolardisorder.

Applicants believe that the Cyclo(hetero)alkenyl Compounds areantagonists for VR1.

The invention relates to methods for inhibiting VR1 function in a cellcomprising contacting a cell capable of expressing VR1 with an effectiveamount of a

Cyclo(hetero)alkenyl Compound. This method can be used in vitro, forexample, as an assay to select cells that express VR1 and, accordingly,are useful as part of an assay to select compounds useful for treatingor preventing pain, UI, an ulcer, IBD, or IBS. The method is also usefulfor inhibiting VR1 function in a cell in vivo, in an animal, a human inone embodiment, by contacting a cell, in an animal, with an effectiveamount of a Cyclo(hetero)alkenyl Compound. In one embodiment, the methodis useful for treating or preventing pain in an animal. In anotherembodiment, the method is useful for treating or preventing UI in ananimal. In another embodiment, the method is useful for treating orpreventing an ulcer in an animal. In another embodiment, the method isuseful for treating or preventing IBD in an animal. In anotherembodiment, the method is useful for treating or preventing IBS in ananimal.

Examples of tissue comprising cells capable of expressing VR1 include,but are not limited to, neuronal, brain, kidney, urothelium, and bladdertissue. Methods for assaying cells that express VR1 are known in theart.

Applicants believe that the Cyclo(hetero)alkenyl Compounds areantagonists for mGluR5.

The invention relates to methods for inhibiting mGluR5 function in acell comprising contacting a cell capable of expressing mGluR5 with anamount of a Cyclo(hetero)alkenyl Compound effective to inhibit mGluR5function in the cell. This method can be used in vitro, for example, asan assay to select cells that express mGluR5 and, accordingly, areuseful as part of an assay to select compounds useful for treating orpreventing pain, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, a pruritic condition, or psychosis. The method isalso useful for inhibiting mGluR5 function in a cell in vivo, in ananimal, a human in one embodiment, by contacting a cell, in an animal,with an amount of a Cyclo(hetero)alkenyl Compound effective to inhibitmGluR5 function in the cell. In one embodiment, the method is useful fortreating or preventing pain in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing an addictivedisorder in an animal in need thereof. In another embodiment, the methodis useful for treating or preventing Parkinson's disease in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing parkinsonism in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing anxiety inan animal in need thereof. In another embodiment, the method is usefulfor treating or preventing a pruritic condition in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing psychosis in an animal in need thereof.

Examples of cells capable of expressing mGluR5 are neuronal and glialcells of the central nervous system, particularly the brain, especiallyin the nucleus accumbens. Methods for assaying cells that express mGluR5are known in the art.

Applicants believe that the Cyclo(hetero)alkenyl Compounds areantagonists for mGluR1.

The invention relates to methods for inhibiting mGluR1 function in acell comprising contacting a cell capable of expressing mGluR1 with anamount of a Cyclo(hetero)alkenyl Compound effective to inhibit mGluR1function in the cell. This method can be used in vitro, for example, asan assay to select cells that express mGluR1 and, accordingly, areuseful as part of an assay to select compounds useful for treating orpreventing pain, UI, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, or depression. Themethod is also useful for inhibiting mGluR1 function in a cell in vivo,in an animal, a human in one embodiment, by contacting a cell, in ananimal, with an amount of a Cyclo(hetero)alkenyl Compound effective toinhibit mGluR1 function in the cell. In one embodiment, the method isuseful for treating or preventing pain in an animal in need thereof. Inanother embodiment, the method is useful for treating or preventing UIin an animal in need thereof. In another embodiment, the method isuseful for treating or preventing an addictive disorder in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing Parkinson's disease in an animal in need thereof. Inanother embodiment, the method is useful for treating or preventingparkinsonism in an animal in need thereof. In another embodiment, themethod is useful for treating or preventing anxiety in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing epilepsy in an animal in need thereof. In another embodiment,the method is useful for treating or preventing stroke in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing a seizure in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing a pruriticcondition in an animal in need thereof. In another embodiment, themethod is useful for treating or preventing psychosis in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing a cognitive disorder in an animal in need thereof. Inanother embodiment, the method is useful for treating or preventing amemory deficit in an animal in need thereof. In another embodiment, themethod is useful for treating or preventing restricted brain function inan animal in need thereof. In another embodiment, the method is usefulfor treating or preventing Huntington's chorea in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing ALS in an animal in need thereof. In another embodiment, themethod is useful for treating or preventing dementia in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing retinopathy in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing a musclespasm in an animal in need thereof. In another embodiment, the method isuseful for treating or preventing a migraine in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing vomiting in an animal in need thereof. In another embodiment,the method is useful for treating or preventing dyskinesia in an animalin need thereof. In another embodiment, the method is useful fortreating or preventing depression in an animal in need thereof.

Examples of cells capable of expressing mGluR1 include, but are notlimited to, cerebellar Purkinje neuron cells, Purkinje cell bodies(punctate), cells of spine(s) of the cerebellum; neurons and neurophilcells of olfactory-bulb glomeruli; cells of the superficial layer of thecerebral cortex; hippocampus cells; thalamus cells; superior colliculuscells; and spinal trigeminal nucleus cells. Methods for assaying cellsthat express mGluR1 are known in the art.

4.5 Therapeutic/Prophylactic Administration and Compositions of theInvention

Due to their activity, the Cyclo(hetero)alkenyl Compounds areadvantageously useful in veterinary and human medicine. As describedabove, the Cyclo(hetero)alkenyl Compounds are useful for treating orpreventing a condition in an animal in need thereof.

When administered to an animal, the Cyclo(hetero)alkenyl Compounds areadministered as a component of a composition that comprises apharmaceutically acceptable carrier or excipient. The presentcompositions, which comprise a Cyclo(hetero)alkenyl Compound, can beadministered orally. The Cyclo(hetero)alkenyl Compounds of the inventioncan also be administered by any other convenient route, for example, byinfusion or bolus injection, by absorption through epithelial ormucocutaneous linings (e.g., oral, rectal, and intestinal mucosa, etc.)and can be administered together with another therapeutically activeagent. Administration can be systemic or local. Various delivery systemsare known, e.g., encapsulation in liposomes, microparticles,microcapsules, capsules, etc., and can be used to administer theCyclo(hetero)alkenyl Compound.

Methods of administration include, but are not limited to, intradermal,intramuscular, intraperitoneal, intravenous, subcutaneous, intranasal,epidural, oral, sublingual, intracerebral, intravaginal, transdermal,rectal, by inhalation, or topical, particularly to the ears, nose, eyes,or skin. The mode of administration is left to the discretion of thepractitioner. In most instances, administration will result in therelease of the Cyclo(hetero)alkenyl Compounds into the bloodstream.

In specific embodiments, it can be desirable to administer theCyclo(hetero)alkenyl Compounds locally. This can be achieved, forexample, and not by way of limitation, by local infusion during surgery,topical application, e.g., in conjunction with a wound dressing aftersurgery, by injection, by means of a catheter, by means of a suppositoryor enema, or by means of an implant, said implant being of a porous,non-porous, or gelatinous material, including membranes, such assialastic membranes, or fibers.

In certain embodiments, it can be desirable to introduce theCyclo(hetero)alkenyl Compounds into the central nervous system orgastrointestinal tract by any suitable route, includingintraventricular, intrathecal, and epidural injection, and enema.Intraventricular injection can be facilitated by an intraventricularcatheter, for example, attached to a reservoir, such as an Ommayareservoir.

Pulmonary administration can also be employed, e.g., by use of aninhaler or nebulizer, and formulation with an aerosolizing agent, or viaperfusion in a fluorocarbon or synthetic pulmonary surfactant. Incertain embodiments, the Cyclo(hetero)alkenyl Compounds can beformulated as a suppository, with traditional binders and excipientssuch as triglycerides.

In another embodiment, the Cyclo(hetero)alkenyl Compounds can bedelivered in a vesicle, in particular a liposome (see Langer, Sci.249:1527-1533 (1990) and Treat et al., Liposomes in the Therapy ofInfectious Disease and Cancer 317-327 and 353-365 (1989)).

In yet another embodiment, the Cyclo(hetero)alkenyl Compounds can bedelivered in a controlled-release system or sustained-release system(see, e.g., Goodson, in Medical Applications of Controlled Release,supra, vol. 2, pp. 115-138 (1984)). Other controlled- orsustained-release systems discussed in the review by Langer, Sci.249:1527-1533 (1990) can be used. In one embodiment, a pump can be used(Langer, Sci. 249:1527-1533 (1990); Sefton, CRC Crit. Ref Biomed. Eng.14:201 (1987); Buchwald et al., Surgery 88:507 (1980); and Saudek etal., N. Engl. J. Med. 321:574 (1989)). In another embodiment, polymericmaterials can be used (see Medical Applications of Controlled Release(Langer and Wise eds., 1974); Controlled Drug Bioavailability, DrugProduct Design and Performance (Smolen and Ball eds., 1984); Ranger andPeppas, J. Macromol. Sci. Rev. Macromol. Chem. 23:61 (1983); Levy etal., Sci. 228:190 (1985); During et al., Ann. Neurol. 25:351 (1989); andHoward et al., J. Neurosurg. 71:105 (1989)). In yet another embodiment,a controlled- or sustained-release system can be placed in proximity ofa target of the Cyclo(hetero)alkenyl Compounds, e.g., the spinal column,brain, or gastrointestinal tract, thus requiring only a fraction of thesystemic dose.

The present compositions can optionally comprise a suitable amount of apharmaceutically acceptable excipient so as to provide the form forproper administration to the animal.

Such pharmaceutical excipients can be liquids, such as water and oils,including those of petroleum, animal, vegetable, or synthetic origin,such as peanut oil, soybean oil, mineral oil, sesame oil and the like.The pharmaceutical excipients can be saline, gum acacia, gelatin, starchpaste, talc, keratin, colloidal silica, urea and the like. In addition,auxiliary, stabilizing, thickening, lubricating, and coloring agents canbe used. In one embodiment, the pharmaceutically acceptable excipientsare sterile when administered to an animal. Water is a particularlyuseful excipient when the Cyclo(hetero)alkenyl Compound is administeredintravenously. Saline solutions and aqueous dextrose and glycerolsolutions can also be employed as liquid excipients, particularly forinjectable solutions. Suitable pharmaceutical excipients also includestarch, glucose, lactose, sucrose, gelatin, malt, rice, flour, chalk,silica gel, sodium stearate, glycerol monostearate, talc, sodiumchloride, dried skim milk, glycerol, propylene, glycol, water, ethanoland the like. The present compositions, if desired, can also containminor amounts of wetting or emulsifying agents, or pH buffering agents.

The present compositions can take the form of solutions, suspensions,emulsions, tablets, pills, pellets, capsules, capsules containingliquids, powders, sustained-release formulations, suppositories,aerosols, sprays, suspensions, or any other form suitable for use. Inone embodiment, the composition is in the form of a capsule (see e.g.,U.S. Pat. No. 5,698,155). Other examples of suitable pharmaceuticalexcipients are described in Remington's Pharmaceutical Sci. 1447-1676(Alfonso R. Gennaro ed., 19th ed. 1995), incorporated herein byreference.

In one embodiment, the Cyclo(hetero)alkenyl Compounds are formulated inaccordance with routine procedures as a composition adapted for oraladministration to human beings. Compositions for oral delivery can be inthe form of tablets, lozenges, aqueous or oily suspensions, granules,powders, emulsions, capsules, syrups, or elixirs, for example. Orallyadministered compositions can contain one or more agents, for example,sweetening agents such as fructose, aspartame or saccharin; flavoringagents such as peppermint, oil of wintergreen, or cherry; coloringagents; and preserving agents, to provide a pharmaceutically palatablepreparation. Moreover, where in tablet or pill form, the compositionscan be coated to delay disintegration and absorption in thegastrointestinal tract thereby providing a sustained action over anextended period of time. Selectively permeable membranes surrounding anosmotically active driving compound are also suitable for orallyadministered compositions. In these latter platforms, fluid from theenvironment surrounding the capsule is imbibed by the driving compound,which swells to displace the agent or agent composition through anaperture. These delivery platforms can provide an essentially zero orderdelivery profile as opposed to the spiked profiles of immediate releaseformulations. A time-delay material such as glycerol monostearate orglycerol stearate can also be used. Oral compositions can includestandard excipients such as mannitol, lactose, starch, magnesiumstearate, sodium saccharin, cellulose, and magnesium carbonate. In oneembodiment, the excipients are of pharmaceutical grade.

In another embodiment, the Cyclo(hetero)alkenyl Compounds can beformulated for intravenous administration. Typically, compositions forintravenous administration comprise sterile isotonic aqueous buffer.Where necessary, the compositions can also include a solubilizing agent.Compositions for intravenous administration can optionally include alocal anesthetic such as lidocaine to lessen pain at the site of theinjection. Generally, the ingredients are supplied either separately ormixed together in unit dosage form, for example, as a dry lyophilizedpowder or water free concentrate in a hermetically sealed container suchas an ampule or sachette indicating the quantity of active agent. Wherethe Cyclo(hetero)alkenyl Compounds are to be administered by infusion,they can be dispensed, for example, with an infusion bottle containingsterile pharmaceutical grade water or saline. Where theCyclo(hetero)alkenyl Compounds are administered by injection, an ampuleof sterile water for injection or saline can be provided so that theingredients can be mixed prior to administration.

The Cyclo(hetero)alkenyl Compounds can be administered bycontrolled-release or sustained-release means or by delivery devicesthat are known to those of ordinary skill in the art. Examples include,but are not limited to, those described in U.S. Pat. Nos. 3,845,770;3,916,899; 3,536,809; 3,598,123; 4,008,719; 5,674,533; 5,059,595;5,591,767; 5,120,548; 5,073,543; 5,639,476; 5,354,556; and 5,733,566,each of which is incorporated herein by reference. Such dosage forms canbe used to provide controlled- or sustained-release of one or moreactive ingredients using, for example, hydropropylmethyl cellulose,other polymer matrices, gels, permeable membranes, osmotic systems,multilayer coatings, microparticles, liposomes, microspheres, or acombination thereof to provide the desired release profile in varyingproportions. Suitable controlled- or sustained-release formulationsknown to those of ordinary skill in the art, including those describedherein, can be readily selected for use with the active ingredients ofthe invention. The invention thus encompasses single unit dosage formssuitable for oral administration such as, but not limited to, tablets,capsules, gelcaps, and caplets that are adapted for controlled- orsustained-release.

Controlled- or sustained-release pharmaceutical compositions can have acommon goal of improving drug therapy over that achieved by theirnon-controlled or non-sustained counterparts. In one embodiment, acontrolled- or sustained-release composition comprises a minimal amountof a Cyclo(hetero)alkenyl Compound to cure or control the condition in aminimum amount of time. Advantages of controlled- or sustained-releasecompositions include extended activity of the drug, reduced dosagefrequency, and increased patient compliance. In addition, controlled- orsustained-release compositions can favorably affect the time of onset ofaction or other characteristics, such as blood levels of theCyclo(hetero)alkenyl Compound, and can thus reduce the occurrence ofadverse side effects.

Controlled- or sustained-release compositions can initially release anamount of a Cyclo(hetero)alkenyl Compound that promptly produces thedesired therapeutic or prophylactic effect, and gradually andcontinually release other amounts of the Cyclo(hetero)alkenyl Compoundto maintain this level of therapeutic or prophylactic effect over anextended period of time. To maintain a constant level of theCyclo(hetero)alkenyl Compound in the body, the Cyclo(hetero)alkenylCompound can be released from the dosage form at a rate that willreplace the amount of Cyclo(hetero)alkenyl Compound being metabolizedand excreted from the body. Controlled- or sustained-release of anactive ingredient can be stimulated by various conditions, including butnot limited to, changes in pH, changes in temperature, concentration oravailability of enzymes, concentration or availability of water, orother physiological conditions or compounds.

In another embodiment, a composition is prepared by admixing aCyclo(hetero)alkenyl Compound or a pharmaceutically acceptable saltthereof and a pharmaceutically acceptable carrier or excipient. Admixingcan be accomplished using methods known for admixing a compound (or asalt) and a pharmaceutically acceptable carrier or excipient. In anotherembodiment; the Cyclo(hetero)alkenyl Compound or a pharmaceuticallyacceptable salt thereof is present in an effective amount.

The amount of the Cyclo(hetero)alkenyl Compound that is effective in thetreatment or prevention of a condition can be determined by standardclinical techniques. In addition, in vitro or in vivo assays canoptionally be employed to help identify optimal dosage ranges. Theprecise dose to be employed will also depend on the route ofadministration, and the seriousness of the Condition and can be decidedaccording to the judgment of a practitioner and and/or each animal'scircumstances. Suitable effective dosage amounts, however, range fromabout 0.01 mg/kg of body weight to about 2500 mg/kg of body weight,although they are typically about 100 mg/kg of body weight or less. Inone embodiment, the effective dosage amount ranges from about 0.01 mg/kgof body weight to about 100 mg/kg of body weight of aCyclo(hetero)alkenyl Compound, in another embodiment, about 0.02 mg/kgof body weight to about 50 mg/kg of body weight, and in anotherembodiment, about 0.025 mg/kg of body weight to about 20 mg/kg of bodyweight. In one embodiment, an effective dosage amount is administeredabout every 24 h until the Condition is abated. In another embodiment,an effective dosage amount is administered about every 12 h until theCondition is abated. In another embodiment, an effective dosage amountis administered about every 8 h until the Condition is abated. Inanother embodiment, an effective dosage amount is administered aboutevery 6 h until the Condition is abated. In another embodiment, aneffective dosage amount is administered about every 4 h until theCondition is abated. The effective dosage amounts described herein referto total amounts administered; that is, if more than oneCyclo(hetero)alkenyl Compound is administered, the effective dosageamounts correspond to the total amount administered.

Where a cell capable of expressing VR1, mGluR5 or mGluR1 is contactedwith a Cyclo(hetero)alkenyl Compound in vitro, the amount effective forinhibiting the VR1, mGluR5 or mGluR1 receptor function in a cell willtypically range from about 0.01 μg/L to about 5 mg/L, in one embodiment,from about 0.01 μg/L to about 2.5 mg/L, in another embodiment, fromabout 0.01 μg/L to about 0.5 mg/L, and in another embodiment, from about0.01 μg/L to about 0.25 mg/L of a solution or suspension of apharmaceutically acceptable carrier or excipient. In one embodiment, thevolume of solution or suspension comprising the Cyclo(hetero)alkenylCompound is from about 0.01 μL to about 1 mL. In another embodiment, thevolume of solution or suspension is about 200 μL.

Where a cell capable of expressing VR1, mGluR5, or mGluR1 is contactedwith a Cyclo(hetero)alkenyl Compound in vivo, the amount effective forinhibiting the receptor function in a cell will typically range fromabout 0.01 mg/kg of body weight to about 100 mg/kg of body weight,although it typically ranges from about 100 mg/kg of body weight orless. In one embodiment, the effective dosage amount ranges from about0.01 mg/kg of body weight to about 100 mg/kg of body weight of aCyclo(hetero)alkenyl Compound, in another embodiment, about 0.020 mg/kgof body weight to about 50 mg/kg of body weight, and in anotherembodiment, about 0.025 mg/kg of body weight to about 20 mg/kg of bodyweight. In one embodiment, an effective dosage amount is administeredabout every 24 h. In another embodiment, an effective dosage amount isadministered about every 12 h. In another embodiment, an effectivedosage amount is administered about every 8 h. In another embodiment, aneffective dosage amount is administered about every 6 h. In anotherembodiment, an effective dosage amount is administered about every 4 h.

The Cyclo(hetero)alkenyl Compounds can be assayed in vitro or in vivofor the desired therapeutic or prophylactic activity prior to use inhumans. Animal model systems can be used to demonstrate safety andefficacy.

The present methods for treating or preventing a Condition in an animalin need thereof can further comprise administering another therapeuticagent to the animal being administered a Cyclo(hetero)alkenyl Compound.In one embodiment, the other therapeutic agent is administered in aneffective amount.

The present methods for inhibiting VR1 function in a cell capable ofexpressing VR1 can further comprise contacting the cell with aneffective amount of another therapeutic agent.

The present methods for inhibiting mGluR5 function in a cell capable ofexpressing mGluR5 can further comprise contacting the cell with aneffective amount of another therapeutic agent.

The present methods for inhibiting mGluR1 function in a cell capable ofexpressing mGluR1 can further comprise contacting the cell with aneffective amount of another therapeutic agent.

Effective amounts of the other therapeutic agents are known to thoseskilled in the art. However, it is well within the skilled artisan'spurview to determine the other therapeutic agent's optimaleffective-amount range. In one embodiment of the invention, whereanother therapeutic agent is administered to an animal, the effectiveamount of the Cyclo(hetero)alkenyl Compound is less than its effectiveamount would be where the other therapeutic agent is not administered.In this case, without being bound by theory, it is believed that theCyclo(hetero)alkenyl Compounds and the other therapeutic agent actsynergistically to treat or prevent a Condition.

The other therapeutic agent can be, but is not limited to, an opioidagonist, a non-opioid analgesic, a non-steroidal anti-inflammatoryagent, an antimigraine agent, a Cox-II inhibitor, an antiemetic, aβ-adrenergic blocker, an anticonvulsant, an antidepressant, aCa2+-channel blocker, an anticancer agent, an agent for treating orpreventing UI, an agent for treating or preventing an ulcer, an agentfor treating or preventing IBD, an agent for treating or preventing IBS,an agent for treating addictive disorder, an agent for treatingParkinson's disease and parkinsonism, an agent for treating anxiety, anagent for treating epilepsy, an agent for treating a stroke, an agentfor treating a seizure, an agent for treating a pruritic condition, anagent for treating psychosis, an agent for treating Huntington's chorea,an agent for treating ALS, an agent for treating a cognitive disorder,an agent for treating a migraine, an agent for treating vomiting, anagent for treating dyskinesia, or an agent for treating depression, andmixtures thereof.

Examples of useful opioid agonists include, but are not limited to,alfentanil, allylprodine, alphaprodine, anileridine, benzylmorphine,bezitramide, buprenorphine, butorphanol, clonitazene, codeine,desomorphine, dextromoramide, dezocine, diampromide, diamorphone,dihydrocodeine, dihydromorphine, dimenoxadol, dimepheptanol,dimethylthiambutene, dioxaphetyl butyrate, dipipanone, eptazocine,ethoheptazine, ethylmethylthiambutene, ethylmorphine, etonitazenefentanyl, heroin, hydrocodone, hydromorphone, hydroxypethidine,isomethadone, ketobemidone, levorphanol, levophenacylmorphan,lofentanil, meperidine, meptazinol, metazocine, methadone, metopon,morphine, myrophine, nalbuphine, narceine, nicomorphine, norlevorphanol,normethadone, nalorphine, normorphine, norpipanone, opium, oxycodone,oxymorphone, papaveretum, pentazocine, phenadoxone, phenomorphan,phenazocine, phenoperidine, piminodine, piritramide, proheptazine,promedol, properidine, propiram, propoxyphene, sufentanil, tilidine,tramadol, pharmaceutically acceptable salts thereof, and mixturesthereof.

In certain embodiments, the opioid agonist is selected from codeine,hydromorphone, hydrocodone, oxycodone, dihydrocodeine, dihydromorphine,morphine, tramadol, oxymorphone, pharmaceutically acceptable saltsthereof, and mixtures thereof.

Examples of useful non-opioid analgesics include non-steroidalanti-inflammatory agents, such as aspirin, ibuprofen, diclofenac,naproxen, benoxaprofen, flurbiprofen, fenoprofen, flubufen, ketoprofen,indoprofen, piroprofen, carprofen, oxaprozin, pramoprofen, muroprofen,trioxaprofen, suprofen, aminoprofen, tiaprofenic acid, fluprofen,bucloxic acid, indomethacin, sulindac, tolmetin, zomepirac, tiopinac,zidometacin, acemetacin, fentiazac, clidanac, oxpinac, mefenamic acid,meclofenamic acid, flufenamic acid, niflumic acid, tolfenamic acid,diflurisal, flufenisal, piroxicam, sudoxicam, isoxicam, andpharmaceutically acceptable salts thereof, and mixtures thereof. Othersuitable non-opioid analgesics include the following, non-limiting,chemical classes of analgesic, antipyretic, nonsteroidalanti-inflammatory drugs: salicylic acid derivatives, including aspirin,sodium salicylate, choline magnesium trisalicylate, salsalate,diflunisal, salicylsalicylic acid, sulfasalazine, and olsalazin;para-aminophenol derivatives including acetaminophen and phenacetin;indole and indene acetic acids, including indomethacin, sulindac, andetodolac; heteroaryl acetic acids, including tolmetin, diclofenac, andketorolac; anthranilic acids (fenamates), including mefenamic acid andmeclofenamic acid; enolic acids, including oxicams (piroxicam,tenoxicam), and pyrazolidinediones (phenylbutazone, oxyphenthartazone);and alkanones, including nabumetone. For a more detailed description ofthe NSAIDs, see Paul A. Insel, Analgesic-Antipyretic andAnti-inflammatory Agents and Drugs Employed in the Treatment of Gout, inGoodman & Gilman's The Pharmacological Basis of Therapeutics 617-57(Perry B. Molinhoff and Raymond W. Ruddon eds., 9^(th) ed 1996) and GlenR. Hanson, Analgesic, Antipyretic and Anti-Inflammatory Drugs inRemington: The Science and Practice of Pharmacy Vol II 1196-1221 (A. R.Gennaro ed. 19th ed. 1995) which are hereby incorporated by reference intheir entireties.

Examples of useful Cox-II inhibitors and 5-lipoxygenase inhibitors, aswell as combinations thereof, are described in U.S. Pat. No. 6,136,839,which is hereby incorporated by reference in its entirety. Examples ofuseful Cox-II inhibitors include, but are not limited to, rofecoxib andcelecoxib.

Examples of useful antimigraine agents include, but are not limited to,alpiropride, bromocriptine, dihydroergotamine, dolasetron, ergocornine,ergocorninine, ergocryptine, ergonovine, ergot, ergotamine, flumedroxoneacetate, fonazine, ketanserin, lisuride, lomerizine, methylergonovine,methysergide, metoprolol, naratriptan, oxetorone, pizotyline,propranolol, risperidone, rizatriptan, sumatriptan, timolol, trazodone,zolmitriptan, and mixtures thereof.

The other therapeutic agent can alternatively be an agent useful forreducing any potential side effects of a Cyclo(hetero)alkenyl Compounds.For example, the other therapeutic agent can be an antiemetic agent.Examples of useful antiemetic agents include, but are not limited to,metoclopromide, domperidone, prochlorperazine, promethazine,chlorpromazine, trimethobenzamide, odansteron, granisetron, hydroxyzine,acetylleucine monoethanolamine, alizapride, azasetron, benzquinamide,bietanautine, bromopride, buclizine, clebopride, cyclizine,dimenhydrinate, diphenidol, dolasetron, meclizine, methallatal,metopimazine, nabilone, oxyperndyl, pipamazine, scopolamine, sulpiride,tetrahydrocannabinol, thiethylperazine, thioproperazine, tropisetron,and mixtures thereof.

Examples of useful β-adrenergic blockers include, but are not limitedto, acebutolol, alprenolol, amosulabol, arotinolol, atenolol, befunolol,betaxolol, bevantolol, bisoprolol, bopindolol, bucumolol, bufetolol,bufuralol, bunitrolol, bupranolol, butidrine hydrochloride, butofilolol,carazolol, carteolol, carvedilol, celiprolol, cetamolol, cloranolol,dilevalol, epanolol, esmolol, indenolol, labetalol, levobunolol,mepindolol, metipranolol, metoprolol, moprolol, nadolol, nadoxolol,nebivalol, nifenalol, nipradilol, oxprenolol, penbutolol, pindolol,practolol, pronethalol, propranolol, sotalol, sulfinalol, talinolol,tertatolol, tilisolol, timolol, toliprolol, and xibenolol.

Examples of useful anticonvulsants include, but are not limited to,acetylpheneturide, albutoin, aloxidone, aminoglutethimide,4-amino-3-hydroxybutyric acid, atrolactamide, beclamide, buramate,calcium bromide, carbamazepine, cinromide, clomethiazole, clonazepam,decimemide, diethadione, dimethadione, doxenitroin, eterobarb,ethadione, ethosuximide, ethotoin, felbamate, fluoresone, gabapentin,5-hydroxytryptophan, lamotrigine, magnesium bromide, magnesium sulfate,mephenytoin, mephobarbital, metharbital, methetoin, methsuximide,5-methyl-5-(3-phenanthryl)-hydantoin, 3-methyl-5-phenylhydantoin,narcobarbital, nimetazepam, nitrazepam, oxcarbazepine, paramethadione,phenacemide, phenetharbital, pheneturide, phenobarbital, phensuximide,phenylmethylbarbituric acid, phenytoin, phethenylate sodium, potassiumbromide, pregabaline, primidone, progabide, sodium bromide, solanum,strontium bromide, suclofenide, sulthiame, tetrantoin, tiagabine,topiramate, trimethadione, valproic acid, valpromide, vigabatrin, andzonisamide.

Examples of useful antidepressants include, but are not limited to,binedaline, caroxazone, citalopram, (S)-citalopram, dimethazan,fencamine, indalpine, indeloxazine hydrocholoride, nefopam, nomifensine,oxitriptan, oxypertine, paroxetine, sertraline, thiazesim, trazodone,benmoxine, iproclozide, iproniazid, isocarboxazid, nialamide, octamoxin,phenelzine, cotinine, rolicyprine, rolipram, maprotiline, metralindole,mianserin, mirtazepine, adinazolam, amitriptyline, amitriptylinoxide,amoxapine, butriptyline, clomipramine, demexiptiline, desipramine,dibenzepin, dimetacrine, dothiepin, doxepin, fluacizine, imipramine,imipramine N-oxide, iprindole, lofepramine, melitracen, metapramine,nortriptyline, noxiptilin, opipramol, pizotyline, propizepine,protriptyline, quinupramine, tianeptine, trimipramine, adrafinil,benactyzine, bupropion, butacetin, dioxadrol, duloxetine, etoperidone,febarbamate, femoxetine, fenpentadiol, fluoxetine, fluvoxamine,hematoporphyrin, hypericin, levophacetoperane, medifoxamine,milnacipran, minaprine, moclobemide, nefazodone, oxaflozane, piberaline,prolintane, pyrisuccideanol, ritanserin, roxindole, rubidium chloride,sulpiride, tandospirone, thozalinone, tofenacin, toloxatone,tranylcypromine, L-tryptophan, venlafaxine, viloxazine, and zimelidine.

Examples of useful Ca2+-channel blockers include, but are not limitedto, bepridil, clentiazem, diltiazem, fendiline, gallopamil, mibefradil,prenylamine, semotiadil, terodiline, verapamil, amlodipine, aranidipine,barnidipine, benidipine, cilnidipine, efonidipine, elgodipine,felodipine, isradipine, lacidipine, lercanidipine, manidipine,nicardipine, nifedipine, nilvadipine, nimodipine, nisoldipine,nitrendipine, cinnarizine, flunarizine, lidoflazine, lomerizine,bencyclane, etafenone, fantofarone, and perhexiline.

Examples of useful anticancer agents include, but are not limited to,acivicin, aclarubicin, acodazole hydrochloride, acronine, adozelesin,aldesleukin, altretamine, ambomycin, ametantrone acetate,aminoglutethimide, amsacrine, anastrozole, anthramycin, asparaginase,asperlin, azacitidine, azetepa, azotomycin, batimastat, benzodepa,bicalutamide, bisantrene hydrochloride, bisnafide dimesylate, bizelesin,bleomycin sulfate, brequinar sodium, bropirimine, busulfan,cactinomycin, calusterone, caracemide, carbetimer, carboplatin,carmustine, carubicin hydrochloride, carzelesin, cedefingol,chlorambucil, cirolemycin, cisplatin, cladribine, crisnatol mesylate,cyclophosphamide, cytarabine, dacarbazine, dactinomycin, daunorubicinhydrochloride, decitabine, dexormaplatin, dezaguanine, dezaguaninemesylate, diaziquone, docetaxel, doxorubicin, doxorubicin hydrochloride,droloxifene, droloxifene citrate, dromostanolone propionate, duazomycin,edatrexate, eflornithine hydrochloride, elsamitrucin, enloplatin,enpromate, epipropidine, epirubicin hydrochloride, erbulozole,esorubicin hydrochloride, estramustine, estramustine phosphate sodium,etanidazole, etoposide, etoposide phosphate, etoprine, fadrozolehydrochloride, fazarabine, fenretinide, floxuridine, fludarabinephosphate, fluorouracil, flurocitabine, fosquidone, fostriecin sodium,gemcitabine, gemcitabine hydrochloride, hydroxyurea, idarubicinhydrochloride, ifosfamide, ilmofosine, interleukin II (includingrecombinant interleukin II or rIL2), interferon alpha-2a, interferonalpha-2b, interferon alpha-n1, interferon alpha-n3, interferon beta-la,interferon gamma-lb, iproplatin, irinotecan hydrochloride, lanreotideacetate, letrozole, leuprolide acetate, liarozole hydrochloride,lometrexol sodium, lomustine, losoxantrone hydrochloride, masoprocol,maytansine, mechlorethamine hydrochloride, megestrol acetate,melengestrol acetate, melphalan, menogaril, mercaptopurine,methotrexate, methotrexate sodium, metoprine, meturedepa, mitindomide,mitocarcin, mitocromin, mitogillin, mitomalcin, mitomycin, mitosper,mitotane, mitoxantrone hydrochloride, mycophenolic acid, nocodazole,nogalamycin, ormaplatin, oxisuran, paclitaxel, pegaspargase, peliomycin,pentamustine, peplomycin sulfate, perfosfamide, pipobroman, piposulfan,piroxantrone hydrochloride, plicamycin, plomestane, porfimer sodium,porfiromycin, prednimustine, procarbazine hydrochloride, puromycin,puromycin hydrochloride, pyrazofurin, riboprine, rogletimide, safingol,safingol hydrochloride, semustine, simtrazene, sparfosate sodium,sparsomycin, spirogermanium hydrochloride, spiromustine, spiroplatin,streptonigrin, streptozotocin, sulofenur, talisomycin, tecogalan sodium,tegafur, teloxantrone hydrochloride, temoporfin, teniposide, teroxirone,testolactone, thiamiprine, thioguanine, thiotepa, tiazofurin,tirapazamine, toremifene citrate, trestolone acetate, triciribinephosphate, trimetrexate, trimetrexate glucuronate, triptorelin,tubulozole hydrochloride, uracil mustard, uredepa, vapreotide,verteporfin, vinblastine sulfate, vincristine sulfate, vindesine,vindesine sulfate, vinepidine sulfate, vinglycinate sulfate,vinleurosine sulfate, vinorelbine tartrate, vinrosidine sulfate,vinzolidine sulfate, vorozole, zeniplatin, zinostatin, zorubicinhydrochloride.

Examples of other anti-cancer drugs include, but are not limited to,20-epi-1,25 dihydroxyvitamin D3; 5-ethynyluracil; abiraterone;aclarubicin; acylfulvene; adecypenol; adozelesin; aldesleukin; ALL-TKantagonists; altretamine; ambamustine; amidox; amifostine;aminolevulinic acid; amrubicin; amsacrine; anagrelide; anastrozole;andrographolide; angiogenesis inhibitors; antagonist D; antagonist G;antarelix; anti-dorsalizing morphogenetic protein-1; antiandrogen,antiestrogen; antineoplaston; antisense oligonucleotides; aphidicolinglycinate; apoptosis gene modulators; apoptosis regulators; apurinicacid; ara-CDP-DL-PTBA; arginine deaminase; asulacrine; atamestane;atrimustine; axinastatin 1; axinastatin 2; axinastatin 3; azasetron;azatoxin; azatyrosine; baccatin III derivatives; balanol; batimastat;BCR/ABL antagonists; benzochlorins; benzoylstaurosporine; beta lactamderivatives; beta-alethine; betaclamycin B; betulinic acid; bFGFinhibitor; bicalutamide; bisantrene; bisaziridinylspermine; bisnafide;bistratene A; bizelesin; breflate; bropirimine; budotitane; buthioninesulfoximine; calcipotriol; calphostin C; camptothecin derivatives;canarypox IL-2; capecitabine; carboxamide-amino-triazole;carboxyamidotriazole; CaRest M3; CARN 700; cartilage derived inhibitor;carzelesin; casein kinase inhibitors (ICOS); castanospermine; cecropinB; cetrorelix; chlorins; chloroquinoxaline sulfonamide; cicaprost;cis-porphyrin; cladribine; clomifene analogues; clotrimazole;collismycin A; collismycin B; combretastatin A4; combretastatinanalogue; conagenin; crambescidin 816; crisnatol; cryptophycin 8;cryptophycin A derivatives; curacin A; cyclopentanthraquinones;cycloplatam; cypemycin; cytarabine ocfosfate; cytolytic factor;cytostatin; dacliximab; decitabine; dehydrodidemnin B; deslorelin;dexamethasone; dexifosfamide; dexrazoxane; dexverapamil; diaziquone;didemnin B; didox; diethylnorspermine; dihydro-5-azacytidine;dihydrotaxol, 9-; dioxamycin; diphenyl spiromustine; docetaxel;docosanol; dolasetron; doxifluridine; droloxifene; dronabinol;duocarmycin SA; ebselen; ecomustine; edelfosine; edrecolomab;eflornithine; elemene; emitefur; epirubicin; epristeride; estramustineanalogue; estrogen agonists; estrogen antagonists; etanidazole;etoposide phosphate; exemestane; fadrozole; fazarabine; fenretinide;filgrastim; finasteride; flavopiridol; flezelastine; fluasterone;fludarabine; fluorodaunorunicin hydrochloride; forfenimex; formestane;fostriecin; fotemustine; gadolinium texaphyrin; gallium nitrate;galocitabine; ganirelix; gelatinase inhibitors; gemcitabine; glutathioneinhibitors; hepsulfam; heregulin; hexamethylene bisacetamide; hypericin;ibandronic acid; idarubicin; idoxifene; idramantone; ilmofosine;ilomastat; imidazoacridones; imiquimod; immunostimulant peptides;insulin-like growth factor-1 receptor inhibitor; interferon agonists;interferons; interleukins; iobenguane; iododoxorubicin; ipomeanol, 4-;iroplact; irsogladine; isobengazole; isohomohalicondrin B; itasetron;jasplakinolide; kahalalide F; lamellarin-N triacetate; lanreotide;leinamycin; lenograstim; lentinan sulfate; leptolstatin; letrozole;leukemia inhibiting factor; leukocyte alpha interferon;leuprolide+estrogen+progesterone; leuprorelin; levamisole; liarozole;linear polyamine analogue; lipophilic disaccharide peptide; lipophilicplatinum compounds; lissoclinamide 7; lobaplatin; lombricine;lometrexol; lonidamine; losoxantrone; lovastatin; loxoribine;lurtotecan; lutetium texaphyrin; lysofylline; lytic peptides;maitansine; mannostatin A; marimastat; masoprocol; maspin; matrilysininhibitors; matrix metalloproteinase inhibitors; menogaril; merbarone;meterelin; methioninase; metoclopramide; MIF inhibitor; mifepristone;miltefosine; mirimostim; mismatched double stranded RNA; mitoguazone;mitolactol; mitomycin analogues; mitonafide; mitotox in fibroblastgrowth factor-saporin; mitoxantrone; mofarotene; molgramostim;monoclonal antibody, human chorionic gonadotrophin; monophosphoryl lipidA+myobacterium cell wall sk; mopidamol; multiple drug resistance geneinhibitor; multiple tumor suppressor 1-based therapy; mustard anticanceragent; mycaperoxide B; mycobacterial cell wall extract; myriaporone;N-acetyldinaline; N-substituted benzamides; nafarelin; nagrestip;naloxone+pentazocine; napavin; naphterpin; nartograstim; nedaplatin;nemorubicin; neridronic acid; neutral endopeptidase; nilutamide;nisamycin; nitric oxide modulators; nitroxide antioxidant; nitrullyn;O6-benzylguanine; octreotide; okicenone; oligonucleotides; onapristone;odansteron; oracin; oral cytokine inducer; ormaplatin; osaterone;oxaliplatin; oxaunomycin; paclitaxel; paclitaxel analogues; paclitaxelderivatives; palauamine; palmitoylrhizoxin; pamidronic acid;panaxytriol; panomifene; parabactin; pazelliptine; pegaspargase;peldesine; pentosan polysulfate sodium; pentostatin; pentrozole;perflubron; perfosfamide; perillyl alcohol; phenazinomycin;phenylacetate; phosphatase inhibitors; picibanil; pilocarpinehydrochloride; pirarubicin; piritrexim; placetin A; placetin B;plasminogen activator inhibitor; platinum complex; platinum compounds;platinum-triamine complex; porfimer sodium; porfiromycin; prednisone;propyl bis-acridone; prostaglandin J2; proteasome inhibitors; proteinA-based immune modulator; protein kinase C inhibitor; protein kinase Cinhibitors, microalgal; protein tyrosine phosphatase inhibitors; purinenucleoside phosphorylase inhibitors; purpurins; pyrazoloacridine;pyridoxylated hemoglobin polyoxyethylene conjugate; raf antagonists;raltitrexed; ramosetron; ras farnesyl protein transferase inhibitors;ras inhibitors; ras-GAP inhibitor; retelliptine demethylated; rhenium Re186 etidronate; rhizoxin; ribozymes; RII retinamide; rogletimide;rohitukine; romurtide; roquinimex; rubiginone B1; ruboxyl; safingol;saintopin; SarCNU; sarcophytol A; sargramostim; Sdi 1 mimetics;semustine; senescence derived inhibitor 1; signal transductioninhibitors; signal transduction modulators; single chain antigen bindingprotein; sizofiran; sobuzoxane; sodium borocaptate; sodiumphenylacetate; solverol; somatomedin binding protein; sonermin;sparfosic acid; spicamycin D; spiromustine; splenopentin; spongistatin1; squalamine; stem cell inhibitor; stem-cell division inhibitors;stipiamide; stromelysin inhibitors; sulfinosine; superactive vasoactiveintestinal peptide antagonist; suradista; suramin; swainsonine;synthetic glycosaminoglycans; tallimustine; tamoxifen methiodide;tauromustine; tazarotene; tecogalan sodium; tegafur; tellurapyrylium;telomerase inhibitors; temoporfin; temozolomide; teniposide;tetrachlorodecaoxide; tetrazomine; thaliblastine; thiocoraline;thrombopoietin; thrombopoietin mimetic; thymalfasin; thymopoietinreceptor agonist; thymotrinan; thyroid stimulating hormone; tin ethyletiopurpurin; tirapazamine; titanocene bichloride; topsentin;toremifene; totipotent stem cell factor; translation inhibitors;tretinoin; triacetyluridine; triciribine; trimetrexate; triptorelin;tropisetron; turosteride; tyrosine kinase inhibitors; tyrphostins; UBCinhibitors; ubenimex; urogenital sinus-derived growth inhibitory factor;urokinase receptor antagonists; vapreotide; variolin B; vector system,erythrocyte gene therapy; velaresol; veramine; verdins; verteporfin;vinorelbine; vinxaltine; vitaxin; vorozole; zanoterone; zeniplatin;zilascorb; and zinostatin stimalamer.

Examples of useful therapeutic agents for treating or preventing UIinclude, but are not limited to, propantheline, imipramine, hyoscyamine,oxybutynin, and dicyclomine.

Examples of useful therapeutic agents for treating or preventing anulcer include, antacids such as aluminum hydroxide, magnesium hydroxide,sodium bicarbonate, and calcium bicarbonate; sucraflate; bismuthcompounds such as bismuth subsalicylate and bismuth subcitrate; H₂antagonists such as cimetidine, ranitidine, famotidine, and nizatidine;H⁺, K⁺-ATPase inhibitors such as omeprazole, iansoprazole, andlansoprazole; carbenoxolone; misprostol; and antibiotics such astetracycline, metronidazole, timidazole, clarithromycin, andamoxicillin.

Examples of useful therapeutic agents for treating or preventing IBDinclude, but are not limited to, anticholinergic drugs; diphenoxylate;loperamide; deodorized opium tincture; codeine; broad-spectrumantibiotics such as metronidazole; sulfasalazine; olsalazine;mesalamine; prednisone; azathioprine; mercaptopurine; and methotrexate.

Examples of useful therapeutic agents for treating or preventing IBSinclude, but are not limited to, propantheline; muscarine receptorantogonists such as pirenzapine, methoctramine, ipratropium, tiotropium,scopolamine, methscopolamine, homatropine, homatropine methylbromide,and methantheline; and antidiarrheal drugs such as diphenoxylate andloperamide.

Examples of useful therapeutic agents for treating or preventing anaddictive disorder include, but are not limited to, methadone,desipramine, amantadine, fluoxetine, buprenorphine, an opiate agonist,3-phenoxypyridine, levomethadyl acetate hydrochloride, and serotoninantagonists.

Examples of useful therapeutic agents for treating or preventingParkinson's disease and parkinsonism include, but are not limited to,carbidopa/levodopa, pergolide, bromocriptine, ropinirole, pramipexole,entacapone, tolcapone, selegiline, amantadine, and trihexyphenidylhydrochloride.

Examples of useful therapeutic agents for treating or preventing anxietyinclude, but are not limited to, benzodiazepines, such as alprazolam,brotizolam, chlordiazepoxide, clobazam, clonazepam, clorazepate,demoxepam, diazepam, estazolam, flumazenil, flurazepam, halazepam,lorazepam, midazolam, nitrazepam, nordazepam, oxazepam, prazepam,quazepam, temazepam, and triazolam; non-benzodiazepine agents, such asbuspirone, gepirone, ipsapirone, tiospirone, zolpicone, zolpidem, andzaleplon; tranquilizers, such as barbituates, e.g., amobarbital,aprobarbital, butabarbital, butalbital, mephobarbital, methohexital,pentobarbital, phenobarbital, secobarbital, and thiopental; andpropanediol carbamates, such as meprobamate and tybamate.

Examples of useful therapeutic agents for treating or preventingepilepsy include, but are not limited to, carbamazepine, ethosuximide,gabapentin, lamotrigine, phenobarbital, phenytoin, primidone, valproicacid, trimethadione, benzodiazepines, vinyl GABA, acetazolamide, andfelbamate.

Examples of useful therapeutic agents for treating or preventing strokeinclude, but are not limited to, anticoagulants such as heparin, agentsthat break up clots such as streptokinase or tissue plasminogenactivator, agents that reduce swelling such as mannitol orcorticosteroids, and acetylsalicylic acid.

Examples of useful therapeutic agents for treating or preventing aseizure include, but are not limited to, carbamazepine, ethosuximide,gabapentin, lamotrigine, phenobarbital, phenytoin, primidone, valproicacid, trimethadione, benzodiazepines, gabapentin, lamotrigine, γ-vinylGABA, acetazolamide, and felbamate.

Examples of useful therapeutic agents for treating or preventing apruritic condition include, but are not limited to, naltrexone;nalmefene; danazol; tricyclics such as amitriptyline, imipramine, anddoxepin; antidepressants such as those given below, menthol; camphor;phenol; pramoxine; capsaicin; tar; steroids; and antihistamines.

Examples of useful therapeutic agents for treating or preventingpsychosis include, but are not limited to, phenothiazines such aschlorpromazine hydrochloride, mesoridazine besylate, and thoridazinehydrochloride; thioxanthenes such as chloroprothixene and thiothixenehydrochloride; clozapine; risperidone; olanzapine; quetiapine;quetiapine fumarate; haloperidol; haloperidol decanoate; loxapinesuccinate; molindone hydrochloride; pimozide; and ziprasidone.

Examples of useful therapeutic agents for treating or preventingHuntington's chorea include, but are not limited to, haloperidol andpimozide.

Examples of useful therapeutic agents for treating or preventing ALSinclude, but are not limited to, baclofen, neurotrophic factors,riluzole, tizanidine, benzodiazepines such as clonazepan and dantrolene.

Examples of useful therapeutic agents for treating or preventingcognitive disorders include, but are not limited to, agents for treatingor preventing dementia such as tacrine; donepezil; ibuprofen;antipsychotic drugs such as thioridazine and haloperidol; andantidepressant drugs such as those given below.

Examples of useful therapeutic agents for treating or preventing amigraine include, but are not limited to, sumatriptan; methysergide;ergotamine; caffeine; and beta-blockers such as propranolol, verapamil,and divalproex.

Examples of useful therapeutic agents for treating or preventingvomiting include, but are not limited to, 5-HT₃ receptor antagonistssuch as odansteron, dolasetron, granisetron, and tropisetron; dopaminereceptor antagonists such as prochlorperazine, thiethylperazine,chlorpromazin, metoclopramide, and domperidone; glucocorticoids such asdexamethasone; and benzodiazepines such as lorazepam and alprazolam.

Examples of useful therapeutic agents for treating or preventingdyskinesia include, but are not limited to, reserpine and tetrabenazine.

Examples of useful therapeutic agents for treating or preventingdepression include, but are not limited to, tricyclic antidepressantssuch as amitryptyline, amoxapine, bupropion, clomipramine, desipramine,doxepin, imipramine, maprotiline, nefazadone, nortriptyline,protriptyline, trazodone, trimipramine, and venlafaxine; selectiveserotonin reuptake inhibitors such as citalopram, (S)-citalopram,fluoxetine, fluvoxamine, paroxetine, and setraline; monoamine oxidaseinhibitors such as isocarboxazid, pargyline, phenelzine, andtranylcypromine; and psychostimulants such as dextroamphetamine andmethylphenidate.

A Cyclo(hetero)alkenyl Compound and the other therapeutic agent can actadditively or in one embodiment, synergistically. In one embodiment, aCyclo(hetero)alkenyl Compound is administered concurrently with anothertherapeutic agent, for example, a composition comprising an effectiveamount of a Cyclo(hetero)alkenyl Compound, an effective amount ofanother therapeutic agent can be administered. Alternatively, acomposition comprising an effective amount of a Cyclo(hetero)alkenylCompound and a different composition comprising an effective amount ofanother therapeutic agent can be concurrently administered. In anotherembodiment, an effective amount of a Cyclo(hetero)alkenyl Compound isadministered prior or subsequent to administration of an effectiveamount of another therapeutic agent. In this embodiment, theCyclo(hetero)alkenyl Compound is administered while the othertherapeutic agent exerts its therapeutic effect, or the othertherapeutic agent is administered while the Cyclo(hetero)alkenylCompound exerts its preventative or therapeutic effect for treating or aCondition.

A composition of the invention is prepared by a method comprisingadmixing a Cyclo(hetero)alkenyl Compound or pharmaceutically acceptablesalt and a pharmaceutically acceptable carrier or excipient. Admixingcan be accomplished using methods well known for admixing a compound (orsalt) and a pharmaceutically acceptable carrier or excipient. In oneembodiment the composition is prepared such that theCyclo(hetero)alkenyl Compound is present in the composition in aneffective amount.

4.6 Kits

The invention encompasses kits that can simplify the administration of aCyclo(hetero)alkenyl Compound to an animal.

A typical kit of the invention comprises a unit dosage form of aCyclo(hetero)alkenyl Compound. In one embodiment, the unit dosage formis a container, which can be sterile, containing an effective amount ofa Cyclo(hetero)alkenyl Compound and a pharmaceutically acceptablecarrier or excipient. The kit can further comprise a label or printedinstructions instructing the use of the Cyclo(hetero)alkenyl Compound totreat or prevent a Condition. The kit can also further comprise a unitdosage form of another therapeutic agent, for example, a secondcontainer containing an effective amount of the other therapeutic agentand a pharmaceutically acceptable carrier or excipient. In anotherembodiment, the kit comprises a container containing an effective amountof a Cyclo(hetero)alkenyl Compound, an effective amount of anothertherapeutic agent and a pharmaceutically acceptable carrier orexcipient. Examples of other therapeutic agents include, but are notlimited to, those listed above.

Kits of the invention can further comprise a device that is useful foradministering the unit dosage forms. Examples of such a device include,but are not limited to, a syringe, a drip bag, a patch, an inhaler, andan enema hag.

The following examples are set forth to assist in understanding theinvention and should not be construed as specifically limiting theinvention described and claimed herein. Such variations of theinvention, including the substitution of all equivalents now known orlater developed, which would be within the purview of those skilled inthe art, and changes in formulation or minor changes in experimentaldesign, are to be considered to fall within the scope of the inventionincorporated herein.

5. EXAMPLES 5.1 Example 1 Synthesis of a Cyclo(Hetero)Alkenyl Compoundof Formula A26(a)

About 1 eq. of 2,3-dichloropyridine A and 1 eq. of a Compound of FormulaB were heated in DMSO (1 mL/mmol) in the presence of about 1 eq. of DIEAat a temperature of about 125° C. for about 12 h. The resulting reactionmixture was cooled to about 25° C. and the solvent was removed underreduced pressure to provide a Compound of Formula C.

The Compound of Formula C was then reacted with 30% TFA in DCM (5mL/mmol) at a temperature of from about 25° C. to about the boilingpoint of the solvent. The resulting reaction mixture was cooled to about25° C., neutralized with aq. Na₂CO₃, and the organic layer separatedfrom the aqueous layer. The aqueous layer was then extracted with DCM,the organic layers combined and dried (MgSO₄), and the solvent removedunder reduced pressure to provide a Compound of Formula D. The Compoundof Formula D was purified using a silica gel column eluted with 15:1hexane-ethyl acetate.

The Compound of Formula D (1 eq.) was reacted with 1.25 eq. of LiHMDS atabout −78° C. and the resulting reaction mixture allowed to stir atabout −78° C. for about 2 h. After stirring for about 2 h, 3 eq. ofN-(5-chloro-2-pyridyl)triflimide 5 was added to the reaction mixture ata temperature of about −78° C. The reaction mixture was then stirred forabout 2.5 h at a temperature of about −78° C. and then allowed to warmto about 25° C. The solvent was removed under reduced pressure and theresulting residue purified using a silica gel column eluted with 20:1hexane-ethyl acetate provide a Compound of Formula E.

The Compound of Formula E (about 1 eq.), 4-(tert-butyl) aniline (about 2eq.), and triethylamine (about 2.2 eq.) were dissolved in DMF (about 1mL/mmol) and the resulting solution was degassed by bubbling N₂ throughthe solution. Pd(OAc)₂ and Dppp (about 0.3 eq. of each) were added tothe solution and the nitrogen atmosphere was replaced with CO at apressure of about 1 atm. The reaction mixture was then heated to about70° C. for about 2 h. The reaction mixture was cooled to about 25° C.and the solvent removed under reduced pressure to provide a residue. Theresulting residue was purified using silica gel column chromatographyeluted with 5:1 hexane-ethyl acetate to provide Cyclo(hetero)alkenylCompound A26(a).

The structure of Cyclo(hetero)alkenyl Compound A26(a) was confirmed by¹H NMR and liquid chromatography-mass spectrometry (LCMS).

Compound of Formula A26(a): ¹H-NMR (CDCl₃): 1.33 (s, 9H), 2.71 (m, 2H),3.60 (t, 2H, J=5.73 Hz), 4.12 (m, 2H), 6.80 (m, 1H), 6.88 (dd, 1H,J=4.9, 7.6 Hz), 7.38 (m, 2H), 7.42 (m, 1H), 7.5 (m, 2H), 7.64 (dd, 1H,J=1.84, 2.02 Hz), 8.21 (dd, 1H, J=1.83, 4.88 Hz); LCMS: 370 (M+1).

5.2 Example 2 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA98(a)

Cyclo(hetero)alkenyl Compound A98(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound A26(a) as describedin Example 1 except that 2-chloro-3-(trifluoromethyl)pyridine was usedin place of 2,3-dichloropyridine.

The structure of Cyclo(hetero)alkenyl Compound A98(a) was confirmed by¹H NMR and liquid chromatography-mass spectrometry.

Compound of Formula A98(a): ¹H NMR (400 MHz, CDCl₃): δ ppm: 1.31 (s,9H), 2.66 (m, 2H), 3.51 (t, 2H), 4.05 (dd, 2H), 6.75 (m, 1H), 6.97 (dd,1H), 7.36 (d, 2H), 7.47 (t, 3H), 7.87 (dd, 1H), 8.41 (dd, 1H); LCMS(M+1): 404.2.

5.3 Example 3 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA34(a)

Cyclo(hetero)alkenyl Compound A34(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound A26(a) as describedin Example 1 except that 4-(trifluoromethyl) aniline was used in placeof 4-(tert-butyl) aniline.

The structure of Cyclo(hetero)alkenyl Compound A34(a) was confirmed by¹H NMR and liquid chromatography-mass spectrometry.

Compound of Formula A34(a): ¹H NMR (400 MHz, CDCl₃) 2.72 (m, 2H), 3.60(t, 2H, J=5.47 Hz), 4.14 (m, 2H), 6.85 (m, 1H), 6.89 (dd, 1H, J=4.58,7.69 Hz), 7.62 (d, 2H, J=8.8 Hz), 7.66 (m, 2H), 7.72 (d, 2H, J=8.3 Hz),8.21 (m, 1H); LCMS: 382 (M+1).

5.4 Example 4 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA29(a)

Cyclo(hetero)alkenyl Compound A29(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound A26(a) as describedin Example 1 except that 4-(iso-propyl) aniline was used in place of4-(tert-butyl) aniline.

Cyclo(hetero)alkenyl Compound A29(a) was confirmed by ¹H NMR and liquidchromatography-mass spectrometry.

Compound of Formula A29(a): ¹H NMR (400 MHz, CD₃OD): δ ppm: 1.21 (bs,6H), 2.61 (bs, 2H), 2.75 (bm, 1H), 3.55 (bs, 2H), 4.12 (bs, 2H), 6.70(s, 1H), 6.82 (m, 1H), 7.21 (t, 2H), 7.40 (s, 1H), 7.45 (t, 2H), 7.77(t, 1H), 8.25 (s, 1H); LCMS: 382 (M+1).

5.5 Example 5 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA75(a)

Cyclo(hetero)alkenyl Compound A75(a) was obtained b_(y) a methodanalogous to that used to obtain the Cyclo(hetero)alkenyl CompoundA26(a) as described in Example 1 except that 2-chloro-3-methyl pyridinewas used in place of 2,3-dichloropyridine and the Compound of Formula Cwas obtained by the following method: 2-chloro-3-methyl pyridine (about1 eq.), a Compound of Formula B (about 1.2 eq.), and sodiumtert-butoxide (1.5 eq.) were dissolved in glyme (0.66 mL/mmol), and theresulting solution was degassed by bubbling N₂ through the solution.

After the solution was degassed, 0.02 eq. of tris-(dibenzylideneacetone)dipalladium (0) catalyst and 0.02 eq. of the ligand depicted below

were added to the solution and the resulting reaction mixture was heatedat a temperature of about 50° C. for about 4.5 h. The reaction mixturewas cooled to about 25° C. and solids removed by filtering over CELITE.The solvent was then removed under reduced pressure to provide aresidue. The resulting residue was purified by column chromatographyusing a silica gel column eluted with 6:1 hexane-ethyl acetate toprovide the Cyclo(hetero)alkenyl Compound A75(a).

The structure of Cyclo(hetero)alkenyl Compound A75(a) was confirmed by¹H NMR and liquid chromatography-mass spectrometry.

Compound of Formula A75(a): ¹H NMR (400 MHz, CDCl₃): 1.33 (s, 9H), 2.33(s, 3H), 2.67 (m, 2H), 3.33 (t, 2H), 3.99 (m, 2H), 6.81 (m, 1H), 6.89(m, 1H), 7.38 (m, 2H), 7.46 (m, 2H), 7.50 (m, 2H), 8.19 (m, 1H); LCMS:350 (M+1).

5.6 Example 6 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA81(a)

Cyclo(hetero)alkenyl Compound A81(a) was obtained by a method analogousto that used to obtain the Cyclo(hetero)alkenyl Compound A75(a) asdescribed in Example 5 except that 4-(isopropoxy) aniline was used inplace of 4-(tert-butyl)aniline.

The structure of Cyclo(hetero)alkenyl Compound A81(a) was confirmed by¹H NMR and liquid chromatography-mass spectrometry.

Compound of Formula A81(a): ¹H NMR (400 MHz, CD₃OD): 1.32 (d, 6H, J=5.98Hz), 2.35 (s, 3H), 2.62 (m, 2H), 3.32 (m, 2H), 3.92 (m, 2H), 4.58 (m,2H), 6.80 (m, 1H), 6.89 (m, 2H), 6.97 (m, 1H), 7.48 (m, 2H), 7.58 (m,1H), 8.1 (m, 1H); LCMS: 351 (M⁺).

5.7 Example 7 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA77(a)

Cyclo(hetero)alkenyl Compound A77(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound A75(a) as describedin Example 5 except that 4-(iso-propyl) aniline was used in place of4-(tert-butyl)aniline.

The structure of Cyclo(hetero)alkenyl Compound A77(a) was confirmed by¹H NMR and mass spectrometry (MS).

Compound of Formula A77(a): ¹H NMR (400 MHz, CD₃OD): δ ppm: 1.25 (bd,6H), 2.22 (s, 3H), 2.61 (bs, 2H), 2.75 (m, 1H), 3.27 (m, 2H), 3.92 (s,2H), 6.71 (s, 1H), 6.85 (m, 1H), 7.23 (t, 2H), 7.52 (bm, 4H), 8.15 (s,1H); MS (EI): m/z 335 (M+1).

5.8 Example 8 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA82(a)

Cyclo(hetero)alkenyl Compound A82(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound A75(a) as describedin Example 5 except that (4-trifluoromethyl) aniline was used in placeof 4-(tert-butyl)aniline.

The structure of Cyclo(hetero)alkenyl Compound A82(a) was confirmed by¹H NMR and liquid chromatography-mass spectrometry.

Compound of Formula A82(a): ¹H NMR (400 MHz, CDCl₃): 2.33 (s, 3H), 2.67(m, 2H), 3.34 (t, 2H, J=5.48 Hz), 4.01 (dd, 2H, J=2.88, 6.16 Hz), 6.86(m, 1H), 6.91 (dd, 1H, J=5.09, 7.5 Hz), 7.46 (m, 1H), 7.62 (d, 2H,J=8.47), 7.65 (b, 1H), 7.73 (d, 2H, J=8.5 Hz), 8.18 (m, 1H); LCMS: 362(M+1).

5.9 Example 9 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA170(a)

A Compound of Formula F (about 1 eq.), a Compound of Formula 2 (about 1eq.) (commercially available from Sigma-Aldrich, St. Louis, Mo.(www.sigma-aldrich.com)), and triethylamine (about 2.2 eq.) weredissolved in DMF (5 mL/mmol) and the resulting solution was stirred atabout 25° C. for about 5 h. The solvent was then removed under reducedpressure to provide a yellow residue. The residue was dissolved inmethylene chloride and filtered through CELITE. The solvent was thenremoved from the resulting filtrate under reduced pressure to provide aCompound of Formula H which was used without further purification. TheCompound of Formula H (about 1 eq.), 4-tert-butyl aniline (about 5 eq.),1-hydroxybenzotriazole (HOBt, about 1 eq.), and DIC (about 1 eq.) weredissolved in DCM and the resulting solution was stirred at about 25° C.for about 2 days. The solvent was removed under reduced pressure and theresulting residue was purified using silica gel column chromatographyeluted with 10:1 hexane-ethyl acetate to provide Cyclo(hetero)alkenylCompound A170(a) as a yellow solid.

The structure of Cyclo(hetero)alkenyl Compound A170(a) was confirmed by¹H NMR and mass spectrometry.

Compound of Formula A170(a): ¹H NMR (400 MHz, CD₃OD): δ ppm: 1.25 (bd,6H), 2.22 (s, 3H), 2.61 (bs, 2H), 2.75 (m, 1H), 3.27 (m, 2H), 3.92 (s,2H), 6.71 (s, 1H), 6.85 (m, 1H), 7.23 (t, 2H), 7.52 (bm, 4H), 8.15 (s,1H); MS (EI): m/z 335 (M+1).

5.10 Example 10 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaB38(a)

Cyclo(hetero)alkenyl Compound B38(a) was obtained by a method analogousto that used to obtain the Cyclo(hetero)alkenyl Compound A26(a) asdescribed in Example 1 except that 0.2 eq. of2-amino-6-methylbenzothiazole was used in place of 0.3 eq.4-(tert-butyl)aniline.

The structure of Cyclo(hetero)alkenyl Compound B38(a) was confirmed by¹H NMR and liquid chromatography-mass spectrometry.

Compound of Formula B38(a): ¹H NMR (400 MHz, CDCl₃): δ ppm: 11.25 (s,1H), 8.15 (dd, 1H), 7.62 (m, 3H), 7.12 (dd, 1H), 6.87 (dd, 1H), 6.81 (m,1H), 3.83 (m, 2H), 3.57 (t, 2H), 2.78 (m, 2H), 2.40 (s, 3H); LCMS(M+H⁺): 385.

5.11 Example 11 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaB37(a)

Cyclo(hetero)alkenyl Compound B37(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound B38(a) as describedin Example 10 except that 2-amino-6-fluorobenzothiazole was used inplace of 2-amino-6-methylbenzothiazole.

The structure of Cyclo(hetero)alkenyl Compound B37(a) was confirmed by¹H NMR and mass spectrometry.

Compound of Formula B37(a): ¹H NMR (400 MHz, DMSO): δ ppm: 2.61 (s, 2H),3.50 (s, 2H), 4.05 (s, 2H), 7.10 (m, 1H), 7.20 (s, 1H), 7.35 (m, 1H),7.75 (m, 1H), 7.80 (t, 1H), 7.92 (m, 1H), 8.23 (s, 1H), 12.20 (s, 1H);MS (EI): m/z 389 (M+1).

5.12 Example 12 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaB85(a) and B84(a)

Cyclo(hetero)alkenyl Compound B85(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound B38(a) as describedin Example 10 except that 2-chloro-3-(trifluoromethyl) pyridine was usedin place 2,3-dichloropyridine.

Cyclo(hetero)alkenyl Compound B84(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound B38(a) as describedin Example 10 except that 2-chloro-3-(trifluoromethyl) pyridine was usedin place 2,3-dichloropyridine, and 2-amino-6-fluorobenzothiazole wasused in place of 2-amino-6-methylbenzothiazole.

The structure of Cyclo(hetero)alkenyl Compound B85(a) was confirmed by¹H NMR and mass spectrometry.

Compound of Formula B85(a): ¹H NMR (CDCl₃): 2.46 (s, 3H), 2.74 (m, 2H),3.54 (t, 2H, J=5.49 Hz), 4.00 (dd, 2H, J=2.86, 6.16 Hz), 6.92 (m, 1H),7.02 (dd, 1H, J=4.16, 8.36 Hz), 7.20 (m, 1H), 7.63 (m, 2H), 7.91 (dd,1H, J=2, 7.96 Hz), 8.44 (m, 1H), 9.90 (b, 1H); MS: 419 (M+1).

The structure of Cyclo(hetero)alkenyl Compound B84(a) was confirmed by¹H NMR and mass spectrometry.

Compound of Formula B84(a): ¹H NMR (400 MHz, CDCl₃): δ ppm: 2.73 (m,2H), 3.52 (t, 2H), 3.95 (d, 2H), 6.90 (s, 1H), 7.06 (m, 2H), 7.51 (dd,1H), 7.65 (dd, 1H), 7.91 (d, 1H), 8.41 (dd, 1H), 10.27 (broad s, 1H);MS: 423.1 (M+1).

5.13 Example 13 Synthesis of a Cyclo(Hetero)Alkenyl Compounds of FormulaB62(a) and B63(a)

Cyclo(hetero)alkenyl Compound B62(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound A75(a) as describedin Example 5 except that 2-amino-6-fluorobenzothiazole was used in place4-(tert-butyl)aniline.

Cyclo(hetero)alkenyl Compound B63(a) was obtained by a method analogousto that used to obtain the Cyclo(hetero)alkenyl Compound A75(a) asdescribed in Example 5 except that 2-amino-6-methylbenzothiazole wasused in place 4-(tert-butyl)aniline.

The structure of Cyclo(hetero)alkenyl Compound B62(a) was confirmed by¹H NMR and mass spectrometry.

Compound of Formula B62(a): ¹H NMR (CDCl₃): 9.82 (br, 1H), 8.17 (dd, 1H,J=1.9 and 4.8 Hz), 7.71 (dd, 1H, J=4.8 and 8.7 Hz), 7.54 (dd, 1H, J=2.6and 8.1 Hz), 7.46 (d, 1H, J=7.2 Hz), 7.15 (ddd, 1H, J=2.3, 6.4 and 8.7Hz), 7.0-7.04 (m, 1H), 6.91 (dd, 1H, J=4.8 and 7.4 Hz), 3.95 (dd, 2H,J=2.8 and 6.4 Hz), 3.35 (dd, 2H, J=5.4 and 5.8 Hz), 2.68-2.74 (m, 2H),2.31 (s, 3H); MS: 369 (M+1).

The structure of Cyclo(hetero)alkenyl Compound B63(a) was confirmed by¹H NMR and mass spectrometry.

Compound of Formula B63(a): ¹H NMR (CDCl₃): 9.80 (br, 1H), 8.19 (dd, 1H,J=1.3 and 4.8 Hz), 7.64-7.66 (m, 2H), 7.45 (d, 1H, J=7.2 Hz), 7.23 (dd,1H, J=1.9 and 8.3 Hz), 6.99-7.0 (m, 1H), 6.85 (dd, 1H, J=4.8 and 7.2Hz), 3.92-3.95 (m, 2H), 3.34 (dd, 2H, 5.4 and 5.5 Hz), 2.68-2.72 (m,2H), 2.48 (s, 3H), 2.31 (s, 3H); MS: 365 (M+1).

5.14 Example 14 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaK1(a)

Cyclo(hetero)alkenyl Compound K1(a) was obtained by a method analogousto that used to obtain Cyclo(hetero)alkenyl Compound A26(a) as describedin Example 1 except that 2,2-difluoro-5-aminobenzodioxole (commerciallyavailable from Lancaster Synthesis of Windam, N.H.) was used in place oftert-butyl aniline.

The structure of Cyclo(hetero)alkenyl Compound K1(a) was confirmed by ¹HNMR.

Compound of Formula K1(a): ¹H NMR (400 MHz, CDCl₃): δ ppm: 8.20-8.17 (m1H), 6.68-7.65 (m, 1H), 7.64-7.61 (m, 1H), 7.43 (bs, 1H), 7.02-6.99 (m,2H), 6.89-6.85 (m, 1H), 6.83-6.78 (m, 1H), 4.14-4.08 (m, 2H), 3.61-3.55(m, 2H), 2.72-2.65 (m, 2H).

5.15 Example 15 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA34(a)

A Compound of Formula C was obtained, in one method, by a methodanalogous to that described in Example 1 except that the heating was ata temperature of about 140° C. for about 12 hours.

A Compound of Formula C was obtained, in another method, by adding at atemperature of about 25° C. the Compound of Formula A (51.9 g, 350 mmol)to a suspension of the Compound of Formula B (50.3 g. 350 mmol) andK₂CO₃ (120 g, 875 mmol) in DMSO to form a reaction mixture. The reactionmixture was stirred at 150° C. for about 16 hours. Thereafter, thereaction mixture was cooled to about 25° C. and quenched with water. Theresulting liquid was extracted 3 times with EtOAc (300 mL perextraction), the organic layers combined and dried (Na₂SO₄), and thesolvent removed to provide the Compound of Formula C (92.5% yield) witha purity of >90%, as determined by LCMS.

The Compound of Formula C (about 0.25 mmol/mL) was reacted with 4N HClin THF at a temperature of about 50° C. for about 16 hours. Theresulting reaction mixture was cooled to about 25° C. and neutralizedwith aqueous Na₂CO₃. Separate aqueous and organic layers formed. Theorganic layer was separated from the aqueous layer. The aqueous layerwas then extracted with about 150-300 mL of ethyl acetate. The organiclayer was combined with the post-extraction ethyl acetate and thecombination was dried with MgSO₄. The solvent was removed under reducedpressure to provide a Compound of Formula D. The Compound of Formula Dwas purified using a silica gel column eluted with 3:1 hexane:ethylacetate (80% yield).

The Compound of Formula D (1 eq., about 0.3 mmol/mL) was reacted with1.2 eq. of aqueous NaCN within the temperature range of from 0° C. to25° C. for about 12 hours. The solvent was removed under reducedpressure and the resulting residue was purified using a silica gelcolumn eluted with 3:1 hexane:ethyl acetate provide a Compound ofFormula J (99% yield).

The Compound of Formula J (about 1 eq., about 0.25 mmol/mL) was reactedwith 2.2 eq. of POCl₃ in pyridine at a temperature of about 25° C. forabout 22 hours. The solvent was removed under reduced pressure and theresulting residue was purified using a silica gel column eluted with 5:1hexane:ethyl acetate provide a Compound of Formula K (91% yield).

The Compound of Formula K (about 0.5 mmol/mL) was refluxed in 6N aqueousHCl at a temperature of about 100° C. for about 12 hours. The resultingreaction mixture was cooled to about 25° C. and the solvent was removedunder reduced pressure to provide a Compound of Formula L which was usedwithout further purification (92% yield).

In a single step procedure, the Compound of Formula L (about 1 eq.),4-trifluoromethyl-aniline (about 1 eq., obtained from Aldrich ChemicalCo., Milwaukee, Wis.), 1-hydroxybenzotriazole (HOBt, about 1.25 eq.),and DIC (about 1.25 eq.) were dissolved in DMF (about 0.35 mmol/mL) andthe resulting solution was stirred at a temperature of about 25° C. forabout 12 hours. The solvent was removed under reduced pressure and theresulting residue was purified using silica gel column chromatographyeluted with 10:1 hexane:ethyl acetate to provide 0.37 equivalents ofCyclo(hetero)alkenyl Compound A34(a) (37% yield).

In a two-step procedure, the Compound of Formula L (about 1 eq., about0.6 mmol/mL) was reacted with excess SOCl₂ (about 24 eq.) at atemperature of about 25° C. for about 12 hours in a first step toprovide a Compound of Formula M, which was used without furtherpurification. Then, in a second step, about 1 equivalent of the Compoundof Formula M (about 1 mmol/5.0 mL), 4-trifluoromethyl-aniline (about 1.5eq.), and triethylamine (about 2.0 eq.) were dissolved in DCM and theresulting solution was degassed by bubbling nitrogen through thesolution. The reaction mixture was kept at about 25° C. for about 4hours. The solvent was removed under reduced pressure to provide aresidue. The resulting residue was purified using a silica gel columnand eluted with 10:1 hexane:ethyl acetate to provide 0.63 equivalents ofCyclo(hetero)alkenyl Compound A34(a) (63% yield for the two-stepprocedure).

The structure of Cyclo(hetero)alkenyl Compound A34(a) was confirmed by¹H-NMR and mass spectrometry.

Compound of Formula A34(a): ¹H-NMR (CDCl₃): 8.19 (dd, 1H, J=1.6, 7.7Hz), 7.73 (d, 2H, J=10.1 Hz), 7.67-7.59 (m, 4H), 6.87 (dd, 1H, J=4.8,7.7 Hz), 6.82 (m, 1H), 4.12 (dd, 2H, J=2.9, 6.3 Hz), 3.58 (t, 2H, J=5.5Hz), 2.70 (m, 2H); MS: 382.1 (M+1).

5.16 Example 16 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA178(a)

Isonicotinic acid N (15 g, 121.8 mmol, obtained from Aldrich ChemicalCo.) was added to about 100 mL of thionyl chloride and the reactionmixture was stirred for about 17 h at about 25° C. After this period,excess SOCl₂ was removed under reduced pressure to provide a whitesolid. About 400 mL of THF was added to the resulting solid and thesolvent was removed under reduced pressure to provide isonicotinic acidchloride as a white powder. The white powder was dissolved in about 400mL of THF. The solution was cooled to about 0° C. and4-trifluoromethyl-aniline (21.6 g, 134.0 mmol, 1.1 eq., obtained fromAldrich Chemical Co.) and sodium bicarbonate (30 g, 365.4 mmol, 3.0 eq.)were added. The reaction mixture was stirred for about 5 min at about 0°C., warmed to about 25° C. over about 30 min, then heated to about 65°C. and kept at that temperature for about 1 h. After this period, thereaction mixture was cooled to about 25° C. and the THF was removedunder reduced pressure. The residue was suspended in about 800 mL ofethyl acetate and washed with about 600 mL of aqueous 3N HCl. Separateaqueous and organic layers formed. The layers were separated and theaqueous layer was extracted three times with about 600 mL of ethylacetate per extraction. The organic layer was combined with thepost-extraction ethyl acetate aliquots. The combination was dried withNa₂SO₄ and the solvent was removed under reduced pressure to provide 32g of the Compound of Formula O as a white solid (99% yield).

The structure of the Compound of Formula O was confirmed by ¹H-NMR andmass spectrometry.

Compound of Formula O: ¹H-NMR (CD₃OD) δ: 9.14-9.08 (m, 2H), 8.60-8.53(m, 2H), 8.06-7.98 (m, 2H), 7.77-7.69 (m, 2H); MS: m/z=267.1.

The Compound of Formula O (31 g, 118.1 mmol) was suspended in a mixtureof THF (400 mL) and DMF (100 mL) at about 25° C. and benzyl bromide(30.3 g, 177.1 mmol, obtained from Aldrich Chemical Co.) was added. Theresulting reaction mixture was refluxed for about 24 hours at atemperature of about 80° C. After this period, the reaction mixture wascooled to about 25° C. and the resulting solid was filtered off. Amajority of the THF was removed from the filtrate under reducedpressure. A precipitate formed when about 400 mL of diethyl ether wasadded to the DMF-enriched solution. The resulting solid was filteredoff. The solids were combined and dried to provide 51 g of the Compoundof Formula P (99% yield).

The structure of the Compound of Formula P was confirmed by ¹H-NMR andmass spectrometry.

Compound of Formula P: ¹H-NMR (CD₃OD) δ: 9.29-9.23 (m, 2H), 8.58-8.51(m, 2H), 7.98-7.92 (m, 2H), 7.72-7.65 (m, 2H), 7.56-7.51 (m, 2H),7.49-7.43 (m, 2H), 5.91 (s, 2H); MS: m/z=357.1.

The Compound of Formula P (48 g, 109.8 mmol) was suspended in about 600mL of methanol, cooled to about 0° C., and sodium borohydride (13.3 g,351.2 mmol) was added in several portions of about 1 g each over aperiod of about 30 min. The reaction mixture was stirred for about 1 hat about 0° C. and warmed to about 25° C. over about a 2 hour period.After this period, the methanol was removed under reduced pressure. Theresidue was diluted with about 800 mL of brine and about 1.5 L of ethylacetate. Separate aqueous and organic layers formed. The layers wereseparated and the aqueous layer was washed twice with about 600 mL ofethyl acetate per wash. The organic layer was combined with thepost-washing ethyl acetate aliquots. The combination was dried withNa₂SO₄ and the solvent was removed under reduced pressure to provide abrown residue. The residue was dissolved in about 200 mL of DCM. Aprecipitate formed when about 200 mL of hexane was added to the DCMsolution. The resulting solid was filtered off. The solid was dried toprovide 39 g of the Compound of Formula Q (98% yield).

The structure of the Compound of Formula Q was confirmed by ¹H-NMR andmass spectrometry.

Compound of Formula Q: ¹H-NMR (CDCl₃) δ: 7.70-7.64 (m, 2H), 7.62-7.56(m, 4H), 7.48 (bs, 1H), 7.38-7.27 (m, 5H), 6.69-6.64 (m, 1H), 3.64 (s,2H), 3.21-3.16 (m, 2H), 2.72-2.66 (m, 2H), 2.56-2.48 (m, 2H); MS:m/z=361.1.

Under a dry nitrogen atmosphere, α-chloroethylchloroformate (16 mL, 22.6g, 158.1 mmol, obtained from Aldrich Chemical Co.) was added drop wiseto a solution of the Compound of Formula Q (30 g, 83.2 mmol) in about500 mL of DCE over a period of about 15 min at about 0° C. The reactionmixture was then warmed to about 25° C. over a period of about 30 min.The reaction mixture was then heated to about 83° C. and refluxed forabout 4 hours at that temperature. After this period, the solvent andunreacted α-chloroethylchloroformate were removed under reducedpressure. The resulting residue was dissolved in about 500 mL ofmethanol. The methanol solution was refluxed for about 3 hours at atemperature of about 65° C. After this, the methanol was removed toprovide 31.3 g of brown residue. The residue was dissolved in about 500mL of DCM. A precipitate formed when about 300 mL of diethyl ether wasadded to the DCM solution. The resulting solid was filtered off. Thesolid was dried to provide 26 g of the Compound of Formula R as whitesolid. The ¹H-NMR and LCMS analyses of the white solid showed that thesample was about 92-95% pure; therefore, the yield (based on thestarting weight of compound Q used) was determined to be about 94-97%.

The structure of the Compound of Formula R was confirmed by ¹H-NMR andmass spectrometry.

Compound of Formula R: ¹H-NMR (CD₃OD) δ: 7.79-7.71 (m, 2H), 7.60-7.49(m, 2H), 6.65-6.59 (m, 1H), 3.84-3.76 (m, 2H), 3.36-3.28 (m, 2H),2.68-2.59 (m, 2H); LCMS: m/z=271.1.

The Compound of Formula R (10.5 g, 34.2 mmol), 2-chloro-3-nitropyridine(5.1 g, 32.2 mmol, obtained from Aldrich Chemical Co.) and triethylamine(19 mL, 13.8 g, 136.8 mmol) were mixed in about 500 mL of DCE at about25° C. and kept for about 12 hours at about 25° C. After this period themixture was poured into about 800 mL of aqueous sodium bicarbonate andabout 800 mL of DCM. Separate aqueous and organic layers formed. Theorganic layer was separated from the aqueous layer. The organic layerwas dried with Na₂SO₄ and the solvent was removed under reduced pressureto provide 14.2 g of crude product. The crude product was dissolved inabout 300 mL of DCM. A precipitate formed when about 600 mL of hexanewas added to the DCM solution. The resulting solid was filtered off anddried to provide 12.5 g of Cyclo(hetero)alkenyl Compound A178(a) as ayellow solid (99% yield).

The structure of Cyclo(hetero)alkenyl Compound A178(a) was confirmed by¹H-NMR and mass spectrometry.

Compound of Formula A178(a): ¹H-NMR (CDCl₃) δ: 8.38-8.35 (m, 1H),8.21-8.16 (m, 2H), 7.73-7.66 (m, 1H), 7.64-7.57 (m, 1H), 7.52 (bs, 1H),6.84-6.79 (m, 1H), 6.75-6.71 (m, 1H), 4.06-4.01 (m, 2H), 3.76-3.70 (m,2H), 2.74-2.67 (m, 2H); MS: m/z=393.1.

5.17 Example 17 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaAAA

A mixture of zinc granules (13.9 g, 212.3 mmol) in ethanol (160 mL),water (40 mL), and HCl (10 mL) was cooled to about 0° C. A solution ofCyclo(hetero)alkenyl Compound A178(a) in about 120 mL of ethanol wasadded to the mixture. The resulting reaction mixture was stirred forabout 1.5 h at about 0° C. After this period, the mixture was filteredand the solvent was removed from the filtrate under reduced pressure toprovide a dark brown residue. The residue was dissolved in about 1 L ofDCM and neutralized with 1N aqueous KOH to a pH of about 10. Separateaqueous and organic layers formed. The organic layer was separated fromthe aqueous layer. The organic layer was dried with Na₂SO₄ and thesolvent was removed under reduced pressure to provide 9.2 g of a brownoil. The ¹H-NMR and LCMS analyses of the oil showed that the sample wasabout 80-85% pure; therefore, the yield (based on the starting weight ofCyclo(hetero)alkenyl Compound AAA) of the Cyclo(hetero)alkenyl CompoundAAA was determined to be about 96-100%.

The structure of Cyclo(hetero)alkenyl Compound AAA was confirmed by¹H-NMR and mass spectrometry.

Compound of Formula AAA: ¹H-NMR (CDCl₃) δ: 7.82-7.79 (m, 1H), 7.73-7.68(m, 2H), 7.63-7.57 (m, 3H), 7.01-6.96 (m, 1H), 6.91-6.83 (m, 2H),3.95-3.89 (m, 2H), 3.83-3.75 (m, 2H), 3.35-129 (m, 2H), 2.68-2.60 (m,2H); LCMS: m/z=363.2.

5.18 Example 18 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA34(a)

Cyclo(hetero)alkenyl Compound AAA (1.77 g, 4.88 mmol) was suspended inabout 100 mL of 6N aqueous HCl, cooled to about 0° C., and treated witha solution of NaNO₂ (0.34 g, 4.88 mmol) in about 40 mL of water withstirring. The resulting solution was stirred for about 30 minutes atabout 0° C. Thereafter, a solution of (CuCl)₂ (0.58 g, 5.86 mmol,obtained from Aldrich Chemical Co.) in about 50 mL of water was added.The resulting mixture was stirred for about 30 minutes at about 0° C.,allowed to warm to about 25° C., then stirred for about 1 h at about 25°C. After this period, the mixture was diluted with about 300 mL of waterand extracted twice with about 700 mL of ethyl acetate used perextraction. The post-extraction ethyl acetate aliquots were combined,dried with Na₂SO₄ and the solvent was removed to provide 1.8 g of a darkbrown oil. This oil was purified by flash chromatography on a silica gelcolumn, using a gradient of from 5:95 to 80:20 (by volume) ethylacetate:hexane as an eluent, to provide 0.82 g of theCyclo(hetero)alkenyl Compound A34(a) as tan solid (45% yield).

The structure of Cyclo(hetero)alkenyl Compound A34(a) was confirmed by¹H-NMR and mass spectrometry.

Compound of Formula A34(a): ¹H-NMR (CDCl₃) δ: 8.19 (dd, 1H, J=1.54, 4.82Hz), 7.73-7.67 (m, 2H), 7.65-7.56 (m, 4H), 6.87 (dd, 1H, J=4.6, 7.45Hz), 6.85-6.82 (m, 1H), 4.14-4.09 (m, 2H), 3.58 (t, 2H, J=5.7 Hz),2.74-2.66 (m, 2H); MS: m/z=382.1.

5.19 Example 19 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA36(a)

Compound A36(a) was prepared according to Example 1, except that4-trifluoromethoxyphenyl amine was used in place of 4-(tert-butyl)aniline.

5.20 Example 20 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaL1(a)

Compound L1(a) was prepared according to Example 1, except that4-chloro-3-trifluoromethylphenyl amine was used in place of4-(tert-butyl) aniline.

5.21 Example 21 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA106(a)

Compound A106(a) was prepared according to Example 3, except that2-chloro-3-trifluoropyridine was used in place of 2,3-dichloropyridine.

5.22 Example 22 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaL3(a)

Compound L3(a) was prepared according to Example 1, except that4-methyl-3-trifluoromethylphenyl amine was used in place of4-(tert-butyl) aniline.

5.23 Example 23 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaL4(a)

Compound L4(a) was prepared according to Example 1, except that3-chloro-4-(trifluoromethylthio)benzenamine was used in place of4-(tert-butyl) aniline.

5.24 Example 24 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaL5(a)

Compound L5(a) was prepared according to Example 1, except that4-fluoro-3-trifluoromethylphenyl amine was used in place of4-(tert-butyl) aniline.

5.25 Example 25 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaL7(a)

Compound L7(a) was prepared according to Example 1, except that4-amino-2-trifluoromethylbenzonitrile was used in place of4-(tert-butyl) aniline.

5.26 Example 26 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA44(a)

Compound A44(a) was prepared according to Example 1, except that4-(1,1,2,2-tetrafluoroethoxy)benzenamine was used in place of4-(tert-butyl) aniline.

5.27 Example 27 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA43(a)

Compound A43(a) was prepared according to Example 1, except thatN,N-diethylbenzene-1,4-diamine was used in place of 4-(tert-butyl)aniline.

5.28 Example 28 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA34(b)

Compound A34(b) was prepared according to Example 1, except that4-trifluoromethylphenyl amine was used in place of 4-(tert-butyl)aniline and 1-(3-chloropyridin-2-yl)-3-methylpiperidin-4-one, thereaction product of 3-methylpiperidin-4-one with 2,3-dichloropyridine(Compound of Formula A), was used in place of the Compound of Formula D.

3-Methylpiperidin-4-one was prepared by debenzylating1-benzyl-3-methylpiperidin-4-one as follows. 70 g (344.3 mmol) of1-benzyl-3-methylpiperidin-4-one (available from Across Organics,Piscataway, N.J.) was dissolved in methanol (400 mL) under a nitrogenatmosphere. 5.6 g of a Pd/C catalyst was added to form a reactionmixture. The nitrogen atmosphere was replaced by a hydrogen atmosphere.The reaction mixture was stirred at 25° C. for 48 hours and thenfiltered through a pad of CELITE (about 200 g). The filtrate wasconcentrated by removing the solvent under reduced pressure to provide38 g of 3-methylpiperidin-4-one.

1-(3-chloropyridin-2-yl)-3-methylpiperidin-4-one was prepared bydissolving 19.2 g 3-methylpiperidin-4-one (168.9 mmol) and 25 g ofCompound of Formula A (168.9 mmol) in DMSO (400 mL) under a nitrogenatmosphere to form a reaction mixture. The reaction mixture was stirredat 85° C. for 12 hours. Therefter, the solvent was removed under reducedpressure. The residue was purified by column chromatography on a silicagel column, using a gradient of from 10:90 to 98:2 (by volume) ethylacetate:hexane as an eluent, to provide 9 g of1-(3-chloropyridin-2-yl)-3-methylpiperidin-4-one.

The structure of Cyclo(hetero)alkenyl Compound A34(b) was confirmed by¹H-NMR.

Compound of Formula A34(b): ¹H NMR (400 MHz, CDCl₃): δ ppm: 8.20 (dd,1H, J=4.82, 1.53 Hz), 7.74-7.69 (m, 2H), 7.64-7.58 (m, 4H), 6.87 (dd,1H, J=7.45, 4.82 Hz), 6.61 (bt, 1H, J=3.29 Hz), 4.17-4.09 (m, 1H), 3.99(td, 1H, J=19.1, 2.85 Hz), 3.64 (dd, 1H, J=12.49, 3.94 Hz), 3.34 (dd,1H, J=12.71, 4.38 Hz), 3.13-3.04 (m, 1H), 1.29 (d, 3H, J=6.79 Hz).

5.29 Example 29 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaK4(a)

Compound K4(a) was prepared according to Example 21, except that2,2-difluoro-5-aminobenzodioxole was used in place of4-(trifluoromethyl) aniline.

5.30 Example 30 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA42(a)

Compound A42(a) was prepared according to Example 1, except that4-(trifluoromethylthio)benzenamine was used in place of 4-(tert-butyl)aniline.

5.31 Example 31 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaM1(a)

Compound M1(a) was prepared according to Example 1, except that5-trifluoromethylpyridin-2-yl amine was used in place of 4-(tert-butyl)aniline.

5.32 Example 32 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaM23(a)

Compound M23(a) was prepared according to Example 1, except that6-trifluoromethylpyridin-3-yl amine was used in place of 4-(tert-butyl)aniline.

5.33 Example 33 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaM4(a)

Compound M4(a) was prepared according to Example 31, except that2-chloro-3-trifluoromethylpyridine was used in place of2,3-dichloropyridine.

5.34 Example 34 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaM26(a)

Compound M26(a) was prepared according to Example 33, except that6-trifluoromethylpyridin-3-yl amine was used in place of5-trifluoromethylpyridin-2-yl amine.

5.35 Example 35 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaE34(a)

Compound E34(a) was prepared according to Example 3, except that2,3-dichloropyrazine was used in place of 2,3-dichloropyridine.

5.36 Example 36 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA58(a)

Compound A58(a) was prepared according to Example 3, except that2-chloro-3-fluoropyridine was used in place of 2,3-dichloropyridine.

5.37 Example 37 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaM2(a)

1.1 eq. of the piperidinyl ketal 1,4-dioxa-8-azaspiro[4.5]-decane (B)was added to a 1.2M solution of 2-chloro-3-fluoropyridine (AAB, 1 eq.)in toluene (96 mL), followed by the addition of 1.1 eq. of the sodiumsalt of 2-methylpropan-2-ol (“NaOtBu”), 0.05 eq. Pd(OAc)₂, and 0.05 eq.Dppp to form a reaction mixture. The atmosphere in contact with thereaction mixture was replaced by nitrogen. The reaction mixture wasstirred with a magnetic stirring bar and heated to 65° C. The reactionmixture was stirred at this temperature for 3 h. The reaction mixturewas then cooled to about 25° C. and filtered through about 200 g ofCELITE powder that had been prewetted with about 200 mL of EtOAc. Thesolvent was partially removed under reduced pressure to provide aresidue. The residue was purified by passing through a silica gel padwith a solution of 50% EtOAc in hexane by volume. This provided theCompound of Formula AAC as a yellow oil (94% yield) which was shown, byLC/MS, to be about 99% pure. The structure of the Compound of FormulaAAC was confirmed by ¹H-NMR spectrometry.

Compound of Formula AAC: ¹H-NMR (CDCl₃) δ: 8.01-7.97 (m, 1H), 7.25-7.17(m, 1H), 6.75-6.69 (m, 1H), 4.02 (s, 4H), 3.64-3.57 (m, 4H), 1.86-1.80(m, 4H).

The Compound of Formula AAC, prepared as described above, was usedwithout further purification. 1 eq. of the Compound of Formula AAC wasdissolved in 60 mL THF. Thereafter, an equal volume of 4N aqueous HClwas added to form a reaction mixture. The reaction mixture was stirredwhile heating to 60° C. and stirred at this temperature for 3 h. Thereaction mixture was then to cooled to about 25° C. The solution wasmade basic by adding aqueous K₂CO₃, extracted with EtOAc, dried overNa₂SO₄, and the solvent was removed under reduced pressure to provide aresidue. The residue was purified by chromatography on a silica gelcolumn, using a gradient of from 0:100 to 5:95 (by volume) methanol:(10%diethyl ether in hexane by volume) as an eluent, to provide, afterremoving the solvent under reduced pressure, the ketone Compound ofFormula AAD as a yellow oil (82% yield). The structure of the Compoundof Formula AAD was confirmed by ¹H-NMR spectrometry.

Compound of Formula AAD: ¹H-NMR (CDCl₃) δ: 8.06-8.01 (m, 1H), 7.33-7.25(m, 1H), 6.85-6.78 (m, 1H), 3.90-3.79 (m, 4H), 2.62-2.51 (m, 4H).

Under a nitrogen atmosphere, the Compound of Formula AAD (5.6 g, 26.6mmol) was dissolved in THF (500 mL) at a temperature of about 25° C. Theresulting solution was cooled to −78° C. and LiHMDS (35 mL, 34.6 mmol,1M in THF) was added to form a reaction mixture. The reaction mixturewas stirred at −78° C. for 1.5 h and a THF (100 mL) solution ofN-(5-chloro-2-pyridyl)triflimide (also known as Comins' reagent, 10.5 g,26.6 mmol) was added. The resulting reaction mixture was stirred at −78°C. for 1 h. The reaction mixture was then warmed to about 25° C. over a1 h period and stirred for an additional 4 h at about 25° C. After thisperiod, the solvent was removed under reduced pressure to provide aresidue. The residue was purified by column chromatography on a silicagel column, using a gradient of from 2:98 to 50:50 (by volume)EtOAc:hexane as an eluent, to provide 5.75 g of the triflate Compound ofFormula AAE as light yellow oil.

The structure of the Compound of Formula AAE was confirmed by ¹H-NMR andmass spectrometry.

Compound of Formula AAE: ¹H-NMR (CDCl₃) δ: 8.03-7.97 (m, 1H), 7.31-7.22(m, 1H+CHCl₃), 6.83-6.75 (m, 1H), 5.92-5.87 (m, 1H), 4.17-4.12 (m, 2H),3.77-3.71 (m, 2H), 2.64-2.58 (m, 2H); MS: 327 (M+1).

Under a nitrogen atmosphere, the Compound of Formula AAE (2.1 g, 6.4mmol), 5-trifluromethyl-pyridin-2-ylamine (AAF, 2.1 g, 12.8 mmol), andtriethylamine (1.96 mL, 1.42 g, 14.2 mmol) were dissolved in THF (30 mL)at a temperature of about 25° C. The resulting solution was stirred for2 min. Thereafter, Pd(OAc)₂ (287 mg, 1.28 mmol) and Dppp (528 mg, 1.28mmol) were added to form a reaction mixture. The reaction mixture wasflushed with nitrogen gas. The nitrogen atmosphere was removed andreplaced by a carbon monoxide atmosphere. The reaction mixture wasstirred while heating to 72° C. and stirred at this temperature for 35minutes. The reaction mixture was then to cooled to about 25° C. Thesolvent was removed under reduced pressure to provide a residue. Theresidue was purified by column chromatography on a silica gel column,using a gradient of from 2:98 to 99:1 (by volume) EtOAc:hexane as aneluent, to provide 1.2 g of Cyclo(hetero)alkenyl Compound M2(a) as awhite solid.

The structure of Cyclo(hetero)alkenyl Compound M2(a) was confirmed by¹H-NMR and mass spectrometry.

Cyclo(hetero)alkenyl Compound M2(a): ¹H-NMR (CD₃OD) δ: 8.66-8.60 (m,1H), 8.40-8.33 (m, 1H), 8.12-7.96 (m, 2H), 7.47-7.36 (m, 1H), 6.95-6.82(m, 2H), 4.26-4.18 (m, 2H), 3.73-3.64 (m, 2H), 2.68-2.57 (m, 2H); MS:m/z=367.

5.38 Example 38 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaY34(a)

Compound Y34(a) was prepared according to Example 3, except that2-chloro-3-fluoropyridine was used in place of 2,3-dichloropyridine.

5.39 Example 39 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaN34(a)

Compound N34(a) was prepared according to Example 1, except that4-(trifluoromethyl)-N-methylbenzenamine was used in place of4-(tert-butyl)aniline.

5.40 Example 40 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA45(a)

Compound A45(a) was prepared according to Example 1, except that2-(4-aminophenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol was used in place of4-(tert-butyl) aniline.

5.41 Example 41 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA226(a)

Compound A226(a) was prepared according to Example 3, except that2-chloro-3-bromopyridine was used in place of 2,3-dichloropyridine.

5.42 Example 42 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaL8(a)

Compound L8(a) was prepared according to Example 1, except that3-chloro-4-trifluoromethoxy aniline was used in place of 4-(tert-butyl)aniline.

5.43 Example 43 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA116(a)

Compound A116(a) was prepared according to Example 33, except that4-(1,1,2,2-tetrafluoroethoxy)phenyl amine was used in place of5-trifluoromethylpyridin-2-yl amine.

5.44 Example 44 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA118(a)

Compound A118(a) was prepared according to Example 1, except that4-(1,1-dimethyl-pentyl)phenyl amine was used in place of 4-(tert-butyl)aniline.

5.45 Example 45 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA120(a)

Compound A120(a) was prepared according to Example 1, except that4-(piperidin-1-yl)benzenamine was used in place of 4-(tert-butyl)aniline.

5.46 Example 46 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaL6(a)

Compound L6(a) was prepared according to Example 1, except that3-fluoro-4-trifluoromethylphenyl amine was used in place of4-(tert-butyl) aniline.

5.47 Example 47 Synthesis of a Cyclo(Hetero)Alkenyl Compound of FormulaA47(a)

Compound A47(a) was prepared according to Example 1, except that2-(4-aminophenyl)-2-methylpropionic acid ethyl ester was used in placeof 4-(tert-butyl)aniline.

5.48 Example 48 Binding of Cyclo(Hetero)Alkenyl Compounds to mGluR5

The following assay can be used to demonstrate that Cyclo(hetero)alkenylCompounds bind to and modulate the activity of mGluR5.

Cell cultures: Primary glial cultures are prepared from cortices ofSprague-Dawley 18 days old embryos. The cortices are dissected and thendissociated by trituration. The resulting cell homogenate is plated ontopoly-D-lysine precoated T175 flasks (BIOCOAT, commercially availablefrom Becton Dickinson and Company Inc. of Franklin Lakes, N.J.) inDulbecco's Modified Eagle's Medium (“DMEM,” pH 7.4), buffered with 25 mMHEPES, and supplemented with 15% fetal calf serum (“FCS,” commerciallyavailable from Hyclone Laboratories Inc. of Omaha, Nebr.), and incubatedat 37° C. and 5% CO₂. After 24 hours, FCS supplementation is reduced to10%. On day six, oligodendrocytes and microglia are removed by stronglytapping the sides of the flasks. One day following this purificationstep, secondary astrocyte cultures are established by subplating onto 96poly-D-lysine precoated T175 flasks (BIOCOAT) at a density of 65,000cells/well in DMEM and 10% FCS. After 24 hours, the astrocytes arewashed with serum free medium and then cultured in DMEM, withoutglutamate, supplemented with 0.5% FCS, 20 mM HEPES, 10 ng/mL epidermalgrowth factor (“EGF”), 1 mM sodium pyruvate, and 1×penicillin/streptomycin at pH 7.5 for 3 to 5 days at 37° C. and 5% CO₂,The procedure allows the expression of the mGluR5 receptor byastrocytes, as demonstrated by S. Miller et al., J. Neurosci.15(9):6103-6109 (1995).

Assay Protocol: After 3-5 days incubation with EGF, the astrocytes arewashed with 127 mM NaCl, 5 mM KCl, 2 mM MgCl₂, 700 mM NaH₂PO₄, 2 mMCaCl₂, 5 mM NaHCO₃, 8 mM HEPES, 10 mM Glucose at pH 7.4 (“Assay Buffer”)and loaded with the dye Fluo-4 (commercially available from MolecularProbes Inc. of Eugene, Oreg.) using 0.1 mL of Assay Buffer containingFluo-4 (3 mM final). After 90 minutes of dye loading, the cells are thenwashed twice with 0.2 mL Assay Buffer and resuspended in 0.1 mL of AssayBuffer. The plates containing the astrocytes are then transferred to aFluorometric Imaging Plate reader (commercially available from MolecularDevices Corporation of Sunnyvale, Calif.) for the assessment of calciummobilization flux in the presence of glutamate and in the presence orabsence of antagonist. After monitoring fluorescence for 15 seconds toestablish a baseline, DMSO solutions containing various concentrationsof a Cyclo(hetero)alkenyl Compound diluted in Assay Buffer (0.05 mL of4× dilutions for competition curves) are added to the cell plate andfluorescence is monitored for 2 minutes. 0.05 mL of a 4× glutamatesolution (agonist) is then added to each well to provide a finalglutamate concentration in each well of 10 mM. Plate fluorescence isthen monitored for an additional 60 seconds after agonist addition. Thefinal DMSO concentration in the assay s is 1.0%. In each experiment,fluorescence is monitored as a function of time and the data analyzedusing Microsoft Excel and GraphPad Prism. Dose-response curves are fitusing a non-linear regression to determine IC₅₀ value. In eachexperiment, each data point is determined two times.

5.49 Example 49 In Vivo Assays for Prevention or Treatment of Pain

Test Animals: Each experiment uses rats weighing between 200-260 g atthe start of the experiment. The rats are group-housed and have freeaccess to food and water at all times, except prior to oraladministration of a Cyclo(hetero)alkenyl Compound when food is removedfor 16 hours before dosing. A control group acts as a comparison to ratstreated with a Cyclo(hetero)alkenyl Compound. The control group isadministered the carrier for the Cyclo(hetero)alkenyl Compound. Thevolume of carrier administered to the control group is the same as thevolume of carrier and Cyclo(hetero)alkenyl Compound administered to thetest group.

Acute Pain: To assess the actions of the Cyclo(hetero)alkenyl Compoundsfor the treatment or prevention of acute pain the rat tail flick testcan be used. Rats are gently restrained by hand and the tail exposed toa focused beam of radiant heat at a point 5 cm from the tip using a tailflick unit (Model 7360, commercially available from Ugo Basile ofItaly). Tail flick latencies are defined as the interval between theonset of the thermal stimulus and the flick of the tail. Animals notresponding within 20 seconds are removed from the tail flick unit andassigned a withdrawal latency of 20 seconds. Tail flick latencies aremeasured immediately before (pre-treatment) and 1, 3, and 5 hoursfollowing administration of a Cyclo(hetero)alkenyl Compound. Data areexpressed as tail flick latency(s) and the percentage of the maximalpossible effect (% MPE), i.e., 15 seconds, is calculated as follows:

${\%\mspace{14mu} M\; P\; E} = {\frac{\left\lbrack {\left( {{post}\mspace{14mu}{administration}{\;\;\;}{latency}} \right) - \left( {{pre}\text{-}{administration}\mspace{14mu}{latency}} \right)} \right\rbrack}{\left( {20\mspace{14mu} s\mspace{14mu}{pre}\text{-}{administation}\mspace{14mu}{latency}} \right)} \times 100}$

The rat tail flick test is described in F. E. D'Amour et al., “A Methodfor Determining Loss of Pain Sensation,” J. Pharmacol. Exp. Ther.72:74-79 (1941).

Acute pain can also be assessed by measuring the animal's response tonoxious mechanical stimuli by determining the paw withdrawal threshold(“PWT”), as described below.

Inflammatory Pain: To assess the actions of the Cyclo(hetero)alkenylCompounds for the treatment or prevention of inflammatory pain theFreund's complete adjuvant (“FCA”) model of inflammatory pain is used.FCA-induced inflammation of the rat hind paw is associated with thedevelopment of persistent inflammatory mechanical hyperalgesia andprovides reliable prediction of the anti-hyperalgesic action ofclinically useful analgesic drugs (L. Bartho et al., “Involvement ofCapsaicin-sensitive Neurones in Hyperalgesia and Enhanced OpioidAntinociception in Inflammation,” Naunyn-Schmiedeberg's Archives ofPharmacol. 342:666-670 (1990)). The left hind paw of each animal isadministered a 50 μL intraplantar injection of 50% FCA. 24 hour postinjection, the animal is assessed for response to noxious mechanicalstimuli by determining the PWT, as described below. Rats are thenadministered a single injection of 1, 3, 10 or 30 mg/Kg of either aCyclo(hetero)alkenyl Compound; 30 mg/Kg of a control selected fromCelebrex, indomethacin or naproxen; or carrier. Responses to noxiousmechanical stimuli are then determined 1, 3, 5 and 24 hours postadministration. Percentage reversal of hyperalgesia for each animal isdefined as:

${\%\mspace{14mu}{Reversal}} = {\frac{\left\lbrack {\left( {{post}\mspace{14mu}{administration}\mspace{14mu} P\; W\; T} \right) - \left( {{pre}\text{-}{administration}\mspace{14mu} P\; W\; T} \right)} \right\rbrack}{\left\lbrack {\left( {{basline}\mspace{14mu} P\; W\; T} \right) - \left( {{pre}\text{-}{administration}\mspace{14mu} P\; W\; T} \right)} \right\rbrack} \times 100}$

Neuropathic Pain: To assess the actions of the Cyclo(hetero)alkenylCompounds for the treatment or prevention of neuropathic pain either theSeltzer model or the Chung model can be used.

In the Seltzer model, the partial sciatic nerve ligation model ofneuropathic pain is used to produce neuropathic hyperalgesia in rats (Z.Seltzer et al., “A Novel Behavioral Model of Neuropathic Pain DisordersProduced in Rats by Partial Sciatic Nerve Injury,” Pain 43:205-218(1990)). Partial ligation of the left sciatic nerve is performed underisoflurane/O₂ inhalation anaesthesia. Following induction of anesthesia,the left thigh of the rat is shaved and the sciatic nerve exposed athigh thigh level through a small incision and is carefully cleared ofsurrounding connective tissues at a site near the trocanther just distalto the point at which the posterior biceps semitendinosus nerve branchesoff of the common sciatic nerve. A 7-0 silk suture is inserted into thenerve with a 3/8 curved, reversed-cutting mini-needle and tightlyligated so that the dorsal ⅓ to ½ of the nerve thickness is held withinthe ligature. The wound is closed with a single muscle suture (4-0 nylon(Vicryl)) and vetbond tissue glue. Following surgery, the wound area isdusted with antibiotic powder. Sham-treated rats undergo an identicalsurgical procedure except that the sciatic nerve is not manipulated.Following surgery, animals are weighed and placed on a warm pad untilthey recover from anesthesia. Animals are then returned to their homecages until behavioral testing begins. The animal is assessed forresponse to noxious mechanical stimuli by determining PWT, as describedbelow, prior to surgery (baseline), then immediately prior to and 1, 3,and 5 hours after drug administration for rear paw of the animal.Percentage reversal of neuropathic hyperalgesia is defined as:

${\%\mspace{14mu}{Reversal}} = {\frac{\left\lbrack {\left( {{post}\mspace{14mu}{administration}\mspace{14mu} P\; W\; T} \right) - \left( {{pre}\text{-}{administration}\mspace{14mu} P\; W\; T} \right)} \right\rbrack}{\left\lbrack {\left( {{basline}\mspace{14mu} P\; W\; T} \right) - \left( {{pre}\text{-}{administration}\mspace{14mu} P\; W\; T} \right)} \right\rbrack} \times 100}$In the Chung model, the spinal nerve ligation model of neuropathic painis used to produce mechanical hyperalgesia, thermal hyperalgesia andtactile allodynia in rats. Surgery is performed under isoflurane/O₂inhalation anaesthesia. Following induction of anaesthesia a 3 cmincision is made and the left paraspinal muscles are separated from thespinous process at the L₄-S₂ levels. The L₆ transverse process iscarefully removed with a pair of small rongeurs to identify visually theL₄-L₆ spinal nerves. The left L₅ (or L₅ and L₆) spinal nerve(s) isisolated and tightly ligated with silk thread. A complete hemostasis isconfirmed and the wound is sutured using non-absorbable sutures, such asnylon sutures or stainless steel staples. Sham-treated rats undergo anidentical surgical procedure except that the spinal nerve(s) is notmanipulated. Following surgery animals are weighed, administered asubcutaneous (s.c.) injection of saline or ringers lactate, the woundarea is dusted with antibiotic powder and they are kept on a warm paduntil they recover from the anesthesia. Animals are then be returned totheir home cages until behavioral testing begins. The animals areassessed for response to noxious mechanical stimuli by determining PWT,as described below, prior to surgery (baseline), then immediately priorto and 1, 3, and 5 hours after being administered a Cyclo(hetero)alkenylCompound for the left rear paw of the animal. The animal can also beassessed for response to noxious thermal stimuli or for tactileallodynia, as described below. The Chung model for neuropathic pain isdescribed in S. H. Kim, “An Experimental Model for Peripheral NeuropathyProduced by Segmental Spinal Nerve Ligation in the Rat,” Pain50(3):355-363 (1992).

Response to Mechanical Stimuli as an Assessment of MechanicalHyperalgesia: The paw pressure assay can be used to assess mechanicalhyperalgesia. For this assay, hind paw withdrawal thresholds (PWT) to anoxious mechanical stimulus are determined using an analgesymeter (Model7200, commercially available from Ugo Basile of Italy) as described inC. Stein, “Unilateral Inflammation of the Hindpaw in Rats as a Model ofProlonged Noxious Stimulation: Alterations in Behavior and NociceptiveThresholds,” Pharmacol. Biochem. and Behavior 31:451-455 (1988). Themaximum weight that can be applied to the hind paw is set at 250 g andthe end point is taken as complete withdrawal of the paw. PWT isdetermined once for each rat at each time point and only the affected(ipsilateral) paw is tested.

Response to Thermal Stimuli as an Assessment of Thermal Hyperalgesia:The plantar test can be used to assess thermal hyperalgesia. For thistest, hind paw withdrawal latencies to a noxious thermal stimulus aredetermined using a plantar test apparatus (commercially available fromUgo Basile of Italy) following the technique described by K. Hargreaveset al., “A New and Sensitive Method for Measuring Thermal Nociception inCutaneous Hyperalgesia,” Pain 32(1):77-88 (1988). The maximum exposuretime is set at 32 seconds to avoid tissue damage and any directed pawwithdrawal from the heat source is taken as the end point Threelatencies are determined at each time point averaged. Only the affected(ipsilateral) paw is tested.

Assessment of Tactile Allodynia: To assess tactile allodynia, rats areplaced in clear, plexiglass compartments with a wire mesh floor andallowed to habituate for a period of at least 15 minutes. Afterhabituation, a series of von Frey monofilaments are presented to theplantar surface of the left (operated) foot of each rat. The series ofvon Frey monofilaments consists of six monofilaments of increasingdiameter, with the smallest diameter fiber presented first. Five trialsare conducted with each filament with each trial separated byapproximately 2 minutes. Each presentation lasts for a period of 4-8seconds or until a nociceptive withdrawal behavior is observed.Flinching, paw withdrawal or licking of the paw are considerednociceptive behavioral responses.

5.50 Example 50 In Vivo Assays for Prevention or Treatment of Anxiety

The elevated plus maze test or the shock-probe burying test can be usedto assess the anxiolytic activity of Cyclo(hetero)alkenyl Compounds inrats or mice.

The Elevated Plus Maze Test: The elevated plus maze consists of aplatform with 4 arms, two open and two closed (50×10×50 cm enclosed withan open roof). Rats (or mice) are placed in the center of the platform,at the crossroad of the 4 arms, facing one of the closed arms. Timespent in the open arms vs the closed arms and number of open arm entriesduring the testing period are recorded. This test is conducted prior todrug administration and again after drug administration. Test resultsare expressed as the mean time spent in open arms and the mean number ofentries into open arms. Known anxiolytic drugs increase both the timespent in open arms and number of open arm entries. The elevated plusmaze test is described in D. Treit, “Animal Models for the Study ofAnti-anxiety Agents: A Review,” Neurosci. & Biobehavioral Reviews9(2):203-222 (1985).

The Shock-Probe Burying Test: For the shock-probe burying test thetesting apparatus consists of a plexiglass box measuring 40×30×40 cm,evenly covered with approximately 5 cm of bedding material (odorabsorbent kitty litter) with a small hole in one end through which ashock probe (6.5 cm long and 0.5 cm in diameter) is inserted. Theplexiglass shock probe is helically wrapped with two copper wiresthrough which an electric current is administered. The current is set at2 mA. Rats are habituated to the testing apparatus for 30 min on 4consecutive days without the shock probe in the box. On test day, ratsare placed in one corner of the test chamber following drugadministration. The probe is not electrified until the rat touches itwith its snout or fore paws, at which point the rat receives a brief 2mA shock. The 15 min testing period begins once the rat receives itsfirst shock and the probe remains electrified for the remainder of thetesting period. The shock elicits burying behavior by the rat. Followingthe first shock, the duration of time the rat spends spraying beddingmaterial toward or over the probe with its snout or fore paws (buryingbehavior) is measured as well as the number of contact-induced shocksthe rat receives from the probe. Known anxiolytic drugs reduce theamount of burying behavior. In addition, an index of the rat'sreactivity to each shock is scored on a 4 point scale. The total timespent immobile during the 15 min testing period is used as an index ofgeneral activity. The shock-probe burying test is described in D. Treit,1985, supra.

5.51 Example 51 In Vivo Assays for Prevention or Treatment of anAddictive Disorder

The conditioned place preference test or drug self-administration testcan be used to assess the ability of Cyclo(hetero)alkenyl Compounds toattenuate the rewarding properties of known drugs of abuse.

The Conditioned Place Preference Test: The apparatus for the conditionedplace preference test consists of two large compartments (45×45×30 cm)made of wood with a plexiglass front wall. These two large compartmentsare distinctly different. Doors at the back of each large compartmentlead to a smaller box (36×18×20 cm) box made of wood, painted grey, witha ceiling of wire mesh. The two large compartments differ in terms ofshading (white vs black), level of illumination (the plexiglass door ofthe white compartment is covered with aluminum foil except for a windowof 7×7 cm), texture (the white compartment has a 3 cm thick floor board(40×40 cm) with nine equally spaced 5 cm diameter holes and the blackhas a wire mesh floor), and olfactory cues (saline in the whitecompartment and 1 mL of 10% acetic acid in the black compartment). Onhabituation and testing days, the doors to the small box remain open,giving the rat free access to both large compartments.

The first session that a rat is placed in the apparatus is a habituationsession and entrances to the smaller grey compartment remain open givingthe rat free access to both large compartments. During habituation, rategenerally show no preference for either compartment. Followinghabituation, rats are given 6 conditioning sessions. Rats are dividedinto 4 groups: carrier pre-treatment+carrier (control group),Cyclo(hetero)alkenyl Compound pre-treatment+carrier, carrierpre-treatment+morphine, Cyclo(hetero)alkenyl Compoundpre-treatment+morphine. During each conditioning session the rat isinjected with one of the drug combinations and confined to onecompartment for 30 min. On the following day, the rat receives acarrier+carrier treatment and is confined to the other largecompartment. Each rat receives three conditioning sessions consisting of3 drug combination-compartment and 3 carrier-compartment pairings. Theorder of injections and the drug/compartment pairings arecounterbalanced within groups. On the test day, rats are injected priorto testing (30 min to 1 hour) with either morphine or carrier and therat is placed in the apparatus, the doors to the grey compartment remainopen and the rat is allowed to explore the entire apparatus for 20 min.The time spent in each compartment is recorded. Known drugs of abuseincrease the time spent in the drug-paired compartment during thetesting session. If the Cyclo(hetero)alkenyl Compound blocks theacquisition of morphine conditioned place preference (reward), therewill be no difference in time spent in each side in rats pre-treatedwith a Cyclo(hetero)alkenyl Compound and the group will not be differentfrom the group of rats that was given carrier+carrier in bothcompartments. Data will be analyzed as time spent in each compartment(drug combination-paired vs carrier-paired). Generally, the experimentis repeated with a minimum of 3 doses of a Cyclo(hetero)alkenylCompound.

The Drug Self-Administration Test: The apparatus for the drugself-administration test is a standard commercially available operantconditioning chamber. Before drug trials begin rats are trained to pressa lever for a food reward. After stable lever pressing behavior isacquired, rats are tested for acquisition of lever pressing for drugreward. Rats are implanted with chronically indwelling jugular cathetersfor i.v. administration of compounds and are allowed to recover for 7days before training begins. Experimental sessions are conducted dailyfor 5 days in 3 hour sessions. Rats are trained to self-administer aknown drug of abuse, such as morphine. Rats are then presented with twolevers, an “active” lever and an “inactive” lever. Pressing of theactive lever results in drug infusion on a fixed ratio 1 (FR1) schedule(i.e., one lever press gives an infusion) followed by a 20 second timeout period (signaled by illumination of a light above the levers).Pressing of the inactive lever results in infusion of excipient.Training continues until the total number of morphine infusionsstabilizes to within ±10% per session. Trained rats are then used toevaluate the effect of Cyclo(hetero)alkenyl Compounds pre-treatment ondrug self-administration. On test day, rats are pre-treated with aCyclo(hetero)alkenyl Compound or excipient and then are allowed toself-administer drug as usual. If the Cyclo(hetero)alkenyl Compoundblocks the rewarding effects of morphine, rats pre-treated with theCyclo(hetero)alkenyl Compound will show a lower rate of respondingcompared to their previous rate of responding and compared to excipientpre-treated rats. Data is analyzed as the change in number of druginfusions per testing session (number of infusions during testsession—number of infusions during training session).

5.52 Example 52 Functional Assay for Characterizing mGluR1 AntagonisticProperties

Functional assays for the characterization of mGluR 1 antagonisticproperties are well known in the art. For example, the followingprocedure can be used.

A CHO-rat mGluR1 cell line is generated using cDNA encoding rat mGluR1receptor (M. Masu and S. Nakanishi, Nature 349:760-765 (1991)). The cDNAencoding rat mGluR1 receptor can be obtained from, e.g., Prof. S.Nakanishi (Kyoto, Japan).

40,000 CHO-rat mGluR1 cells/well are plated into a COSTAR 3409, black,clear bottom, 96 well, tissue culture treated plate (commerciallyavailable from Fisher Scientific of Chicago, Ill.) and are incubated inDulbecco's Modified Eagle's Medium (DMEM, pH 7.4) supplemented withglutamine, 10% FBS, 1% Pen/Strep, and 500 μg/mL Geneticin for about 12h. The CHO-rat mGluR1 cells are then washed and treated with OPTIMEMmedium (commercially available from Invitrogen, Carlsbad, Calif.) andincubated for a time period ranging from 1 to 4 hours prior to loadingthe cells with the dye FLUO-4 (commercially available from MolecularProbes Inc., Eugene, Oreg.). After incubation, the cell plates arewashed with loading buffer (127 mM NaCl, 5 mM KCl, 2 mM MgCl₂, 700 μM,NaH₂PO₄, 2 mM CaCl₂, 5 mMNaHCO₃, 8 mM HEPES, and 10 mM glucose, pH 7.4)and incubated with 3 μM FLUO-4 in 0.1 mL loading buffer for 90 min. Thecells are then washed twice with 0.2 mL loading buffer, resuspended in0.1 mL of loading buffer, and transferred to a Fluorometric ImagingPlate Reader (“FLIPR”) (commercially available from Molecular DevicesCorp., Sunnyvale, Calif.) for measurement of calcium mobilization fluxin the presence of glutamate and in the presence or absence of aCyclo(hetero)alkenyl Compound.

To measure calcium mobilization flux, fluoresence is monitored for about15 s to establish a baseline and DMSO solutions containing variousconcentrations of a Cyclo(hetero)alkenyl Compound ranging from about 50μM to about 0.8 nM diluted in loading buffer (0.05 mL of a 4× dilution)are added to the cell plate and fluoresence is monitored for about 2min. 0.05 mL of a 4× glutamate solution (agonist) is then added to eachwell to provide a final glutamate concentration in each well of 10 μMand fluoresence is monitored for about 1 additional min. The final DMSOconcentration in the assay is 1%. In each experiment fluoresence ismonitored as a function of time and the data is analyzed using anon-linear regression to determine the IC₅₀ value. In each experimenteach data point is determined twice.

5.53 Example 53 Binding of Cyclo(Hetero)Alkenyl Compounds to VR1

Methods for demonstrating a compound's ability to inhibit VR1 are knownto those skilled in the art, for example, those methods disclosed inU.S. Pat. No. 6,239,267 to Duckworth et al.; U.S. Pat. No. 6,406,908 toMcIntyre et al.; or U.S. Pat. No. 6,335,180 to Julius et al.

Binding of Compound A77(a) to VR1: Assay Protocol

Human VR1 cloning. Human spinal cord RNA (commercially available fromClontech, Palo Alto, Calif.) was used. Reverse transcription wasconducted on 1.0 μg total RNA using Thermoscript Reverse Transcriptase(commercially available from Invitrogen, Carlsbad, Calif.) and oligo dTprimers as detailed in its product description. Reverse transcriptionreactions were incubated at 55° C. for 1 h, heat-inactivated at 85° C.for 5 min, and RNase H-treated at 37° C. for 20 min.

Human VR1 cDNA sequence was obtained by comparison of the human genomicsequence, prior to annotation, to the published rat sequence. Intronsequences were removed and flanking exonic sequences were joined togenerate the hypothetical human cDNA. Primers flanking the coding regionof human. VR1 were designed as follows: forward primer,AAGATCTTCGCTGGTTGCACACTGGGCCACA (SEQ ID NO:1); and reverse primer,GAAGATCTTCGGGGACAGTGACGGTTGGATGT (SEQ ID NO:2).

PCR of VR1 was performed on one tenth of the Reverse transcriptionreaction mixture using Expand Long Template Polymerase and Expand Buffer2 in a final volume of 50 μL according to the manufacturer'sinstructions (Roche Applied Sciences, Indianapolis, Ind.). Afterdenaturation at 94° C. for 2 min PCR amplification was performed for 25cycles at 94° C. for 15 sec, 58° C. for 30 sec, and 68° C. for 3 minfollowed by a final incubation at 72° C. for 7 min to complete theamplification. A PCR product of ˜2.8 kb was gel-isolated using a 1.0%agarose, Tris-Acetate gel containing 1.6 μg/mL of crystal violet andpurified with a S.N.A.P. UV-Free Gel Purification Kit (commerciallyavailable from Invitrogen). The VR1 PCR product was cloned into thepIND/V5-His-TOPO vector (commercially available from Invitrogen)according to the manufacturer's instructions. DNA preparations,restriction enzyme digestions, and preliminary DNA sequencing wereperformed according to standard protocols. Full-length sequencingconfirmed the identity of the human VR1.

Generation of inducible cell lines. Unless noted otherwise, cell culturereagents were purchased from Life Technologies of Rockville, Md.HEK293-EcR cells expressing the ecdysone receptor (commerciallyavailable from Invitrogen) were cultured in Growth Medium (Dulbecco'sModified Eagles Medium containing 10% fetal bovine serum (commerciallyavailable from HYCLONE, Logan, Utah), 1× penicillin/streptomycin, 1×glutamine, 1 mM sodium pyruvate and 400 μg/mL Zeocin (commerciallyavailable from Invitrogen)). The VR1-pIND constructs were transfectedinto the HEK293-EcR cell line using Fugene transfection reagent(commercially available from Roche Applied Sciences, Basel,Switzerland). After 48 h, cells were transferred to Selection Medium(Growth Medium containing 300 μg/mL G418 (commercially available fromInvitrogen)). Approximately 3 weeks later individual Zeocin/G418resistant colonies were isolated and expanded. To identify functionalclones, multiple colonies were plated into 96-well plates and expressionwas induced for 48 h using Selection Medium supplemented with 5 μMponasterone A (“PonA”) (commercially available from Invitrogen). On theday of assay, cells were loaded with Fluo-4 (a calcium-sensitive dyethat is commercially available from Molecular Probes, Eugene, Oreg.) andCAP-mediated calcium influx was measured using a FLIPR as describedbelow. Functional clones were re-assayed, expanded, and cryopreserved.

pH-Based Assay. Two days prior to performing this assay, cells wereseeded on poly-D-lysine-coated 96-well clear-bottom black plates(commercially available from Becton-Dickinson) at 75,000 cells/well ingrowth media containing 5 μM PonA (commercially available fromInvitrogen) to induce expression. On the day of the assay, the plateswere washed with 0.2 mL 1× Hank's Balanced Salt Solution (commerciallyavailable from Life Technologies) containing 1.6 mM CaCl₂ and 20 mMHEPES, pH 7.4 (“wash buffer”), and loaded using 0.1 mL of wash buffercontaining Fluo-4 (3 μM final concentration, commercially available fromMolecular Probes). After 1 h, the cells were washed twice with 0.2 mLwash buffer and resuspended in 0.05 mL 1× Hank's Balanced Salt Solution(commercially available from Life Technologies) containing 3.5 mM CaCl₂and 10 mM Citrate, pH 7.4 (“assay buffer”). Plates were then transferredto a FLIPR for assay. Compound A77(a) was diluted in assay buffer, and50 mL of the resultant solution were added to the cell plates and thesolution monitored for two minutes. The final concentration of CompoundA77(a) ranged from about 50 pM to about 3 μM. Agonist buffer (washbuffer titrated with 1N HCl to provide a solution having a pH of 5.5when mixed 1:1 with assay buffer) (0.1 mL) was then added to each well,and the plates were incubated for 1 additional min. Data were collectedover the entire time course and analyzed using Excel and Graph PadPrism. Compound A77(a) when assayed according to this protocol had anIC₅₀ of 148.1 nM.

Capsaicin-based Assay. Two days prior to performing this assay, cellswere seeded in poly-D-lysine-coated 96-well clear-bottom black plates(50,000 cells/well) in growth media containing 5 μM PonA (commerciallyavailable from Invitrogen) to induce expression. On the day of theassay, the plates were washed with 0.2 mL 1× Hank's Balanced SaltSolution (commercially available from Life Technologies) containing 1 mMCaCl₂ and 20 mM HEPES, pH 7.4, and cells were loaded using 0.1 mL ofwash buffer containing Fluo-4 (3 μM final). After one h, the cells werewashed twice with 0.2 mL of wash buffer and resuspended in 0.1 mL ofwash buffer. The plates were transferred to a FLIPR for assay. 50 μL ofCompound A77(a) diluted with assay buffer were added to the cell platesand incubated for 2 min. The final concentration of Compound A77(a)ranged from about 50 pM to about 3 μM. Human VR1 was activated by theaddition of 50 μL of capsaicin (400 nM), and the plates were incubatedfor an additional 3 min. Data were collected over the entire time courseand analyzed using Excel and GraphPad Prism. Compound A77(a) whenassayed according to this protocol had an IC₅₀ of 4.4 nM.

The results of the pH-based assay and the capsaicin-based assaydemonstrate that Compound A77(a), an illustrative Cyclo(hetero)alkenylCompound, binds to and modulates the activity of human VR1 and,accordingly, is useful for treating or preventing pain, UI, an ulcer,IBD or IBS.

The present invention is not to be limited in scope by the specificembodiments disclosed in the examples which are intended asillustrations of a few aspects of the invention and any embodiments thatare functionally equivalent are within the scope of this invention.Indeed, various modifications of the invention in addition to thoseshown and described herein will become apparent to those skilled in theart and are intended to fall within the scope of the appended claims.

A number of references have been cited, the entire disclosures of whichare incorporated herein by reference.

1. A compound of formula:

or a pharmaceutically acceptable salt thereof, wherein Ar¹ is

Ar² is

V is CH; X is O or S; Y₁ and Y₂ are —CH₂— and —CH₂—, —O— and —O—, —NH— and —NH—, —S— and —S—, —CH₂— and —O—, —CH₂— and —NH—, —CH₂— and —S—, —O— and —CH₂—, —NH— and —CH₂—, —S— and —CH₂—, —O— and —NH—, —NH— and —O—, —S— and —NH—, or —NH— and —S— respectively; R₁ is —H, —(C₁-C₄)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂, C(halo)₃, —CH(halo)₂, or —CH₂(halo); each R₂ is independently: (a) -halo, —CN, —OH, —NO₂, or —NH₂, (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups, or (c)-phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered)heteroaryl, each of which is unsubstituted or substituted with one or more R₆ groups; each R₃ is independently: (a) -halo, —CN, —OH, —NO₂, or —NH₂, (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups, or (c)-phenyl, -naphthyl, —(C₁₄)aryl or -(5- to 10-membered) heteroaryl, each of which is unsubstituted or substituted with one or more R₆ groups; R₄ is —H or —(C₁-C₆)alkyl; each R₅ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3- to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cyeloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, -(3- to 5-membered)heterocycle, —C(halo)₃, —CH(halo)₂, or CH₂(halo); each R₈ is independently —H, —(C₁-C₁₀)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, —S(O)₂R₇, —R₇OR₇, —R₇COR₇, —R₇C(O)OR₇, —R₇OC(O)R₇, —R₇OC(O)OR₇, —R₇SR₇, —R₇S(O)R₇, —R₇S(O)₂R₇, —C(halo)₂C(halo)₃, —C(halo)₂CH(halo)₂, —CH(C(halo)₃)₂, —CH(C(halo)₃)(CH₃), —OC(halo)₂C(halo)₃, —OC(halo)₂CH(halo)₂, —OCH(C(halo)₃)₂, —OCH(C(halo)₃)(CH₃), —C(OH)(CF₃)₂, —(C₁-C₁₀)alkyl, or -(3- to 7-membered)heterocycle; each R₉ is independently —H, -halo or —(C₁-C₆)alkyl; each R₁₁ is independently —CN, —OH, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, or —OC(O)OR₇; each halo is independently —F, —Cl, —Br, or —I; m is 0 or 1 and when m is 1, R₃ is attached to the 2-, 3-, 5-, or 6-position of the cyclo(hetero)alkenyl ring; n is an integer ranging from 0 to 3; p is an integer ranging from 0 to 2; q is an integer ranging from 0 to 6; r is an integer ranging from 0 to 5; and s is an integer ranging from 0 to
 4. 2. The compound of claim 1, wherein Ar² is


3. The compound of claim 1, wherein Ar¹ is


4. The compound of claim 1, wherein each R₈ is independently —(C₁-C₆)alkyl, —(C₂—-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.
 5. The compound of claim 3, wherein each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.
 6. The compound of claim 1, wherein R₄ is —H; R₁ is —H, -halo, —CH₃, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃, —CH(halo)₂, or —CH₂(halo); and each R₈ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₈-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇.
 7. The compound of claim 6, wherein n or p is 1 and R₂ is —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups.
 8. The compound of claim 6, wherein X is O.
 9. The compound of claim 6, wherein Ar¹ is pyridyl; n is 1 and R₂ is —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups.
 10. The compound of claim 8, wherein m is 0; n is 0; V is N; and Ar¹ is


11. The compound of claim 10, wherein R₁ is Cl, Ar² is


12. The compound of claim 11, wherein r is 1 and R₈ is halo or —(C₁-C₆)alkyl.
 13. The compound of claim 12, wherein Ar² is substituted in the 4-position.
 14. The compound of claim 13, wherein the —(C₁-C₆)alkyl is tert-butyl group.
 15. The compound of claim 13, wherein R₈ is halo.
 16. The compound of claim 8, wherein n is 0, m is 1, R₁ is —CH₃, and Ar¹ is pyridyl.
 17. The compound of claim 16, wherein Ar² is


18. The compound of claim 17, wherein r is 1 and R₈ is halo or —(C₁-C₆)alkyl.
 19. The compound of claim 17, wherein the —(C₁-C₆)alkyl is tert-butyl group and Ar² is substituted at 4-position.
 20. The compound of claim 17, wherein R₈ is halo.
 21. The compound of claim 8, wherein Ar¹ is

Ar² is


22. The compound of claim 21, wherein n is 1 and R₂ is —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups.
 23. The compound of claim 21, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; r is 1 and R₈ is -halo.
 24. The compound of claim 21, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; r is 1 and R₈ is —CF₃.
 25. The compound of claim 21, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; r is 1 and R₈ is -tert-butyl.
 26. The compound of claim 21, wherein R₁ is —CF₃; n is 0; r is 1 and R₈ is -tert-butyl.
 27. The compound of claim 21, wherein R₁ is —CH₃; n is 0; r is 1 and R₈ is -halo.
 28. The compound of claim 21, wherein R₁ is —CF₃; n is 0; r is 1 and R₈ is -halo.
 29. The compound of claim 21, wherein R₁ is —CF₃; n is 0; r is 1 and R₈ is —CH₃.
 30. The compound of claim 21, wherein n is 0; m is 0; R₁ is —CH₃; r is 1 and R₈ is —CF₃.
 31. The compound of claim 21, wherein R₁ is —CF₃; n is 0; r is 1 and R₈ is —CF₃.
 32. The compound of claim 21, wherein R₁ is —CH₃; n is 0; r is 1 and R₈ is -tert-butyl.
 33. The compound of claim 8, wherein Ar¹ is

and Ar² is


34. The compound of claim 33, wherein n is 1 and R₂ is —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups.
 35. The compound of claim 33, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; s is 1 and R₈ is -halo.
 36. The compound of claim 33, wherein R₁ is —CH₃; n is 0; s is 1 and R₈ is -halo.
 37. The compound of claim 33, wherein R₁ is —CF₃; n is 0; s is 1 and R₈ is -halo.
 38. The compound of claim 33, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; s is 1 and R₈ is —CH₃.
 39. The compound of claim 33, wherein R₁ is —CH₃; n is 0; s is 1 and R₈ is —CH₃.
 40. The compound of claim 33, wherein R₁ is —CF₃; n is 0; s is 1 and R₈ is —CH₃.
 41. The compound of claim 33, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; s is 1 and R₈ is —CF₃.
 42. The compound of claim 33, wherein R₁ is —CH₃; n is 0; s is 1 and R₈ is —CF₃.
 43. The compound of claim 33, wherein R₁ is —CF₃; n is 0; s is 1 and R₈ is —CF₃.
 44. The compound of claim 33, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; s is 1 and R₈ is —CH₂CF₃.
 45. The compound of claim 33, wherein R₁ is —CH₃; n is 0; s is 1 and R₈ is —CH₂CF₃.
 46. The compound of claim 33, wherein R₁ is —CF₃; n is 0; s is 1 and R₈ is —CH₂CF₃.
 47. The compound of claim 33, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; s is 1 and R₈ is -tert-butyl.
 48. The compound of claim 33, wherein R₁ is —CF₃, n is 0; s is 1 and R₈ is -tert-butyl.
 49. The compound of claim 10, wherein Ar² is


50. The compound of claim 49, wherein R₁ is —F, —Cl, —Br, or —I; s is 1 and R₈ is -halo.
 51. The compound of claim 49, wherein R₁ is —F, —Cl, —Br, or —I; s is 1 and R₈ is —CF₃.
 52. The compound of claim 49, wherein R₁ is —F, —Cl, —Br, or —I; and R₈ is -tert-butyl.
 53. The compound of claim 49, wherein R₁ is —CF₃; s is 1 and R₈ is -halo.
 54. The compound of claim 49, wherein R₁ is —CF₃; s is 1 and R₈ is —CF₃.
 55. The compound of claim 49, wherein R₁ is —CF₃, s is 1 and R₈ is -tert-butyl.
 56. The compound of claim 49, wherein R₁ is —CH₃; s is 1 and R₈ is -halo.
 57. The compound of claim 49, wherein R₁ is —CF₃; s is 1 and R₈ is —CH₃.
 58. The compound of claim 49, wherein R₁ is —CH₃; s is 1 and R₈ is —CF₃.
 59. The compound of claim 49, wherein R₁ is —CH₃, s is 1 and R₈ is -tert-butyl.
 60. The compound of claim 8, wherein m is 0; Ar¹ is

and Ar² is


61. The compound of claim 60, wherein R₁ is —F, —Cl, —Br, or —I; s is 1; n is 0; and R₈ is -halo.
 62. The compound of claim 60, wherein R₁ is —F, —Cl, —Br, or —I; s is 1; n is 0; and R₈ is —CF₃.
 63. The compound of claim 60, wherein R₁ is —F, —Cl, —Br, or —I; s is 1; n is 0; and R₈ is -tert-butyl.
 64. The compound of claim 60, wherein R₁ is —CF₃; s is 1; n is 0; and R₈ is -halo.
 65. The compound of claim 60, wherein R₁ is —CF₃; s is 1; n is 0; and R₈ is —CF₃.
 66. The compound of claim 60, wherein R₁ is —CF₃; Ar² is s is 1; n is 0; and R₈ is -tert-butyl.
 67. The compound of claim 60, wherein R₁ is —CH₃; s is 1; n is 0; and R₈ is -halo.
 68. The compound of claim 60, wherein R₁ is —CF₃; s is 1; n is 0; and R₈ is —CH₃.
 69. The compound of claim 60, wherein R₁ is —CH₃; s is 1; n is 0; and R₈ is —CF₃.
 70. The compound of claim 60, wherein R₁ is —CH₃; s is 1; n is 0; and R₈ is -tert-butyl.
 71. The compound of claim 8, wherein m is 0; Ar¹ is

and Ar² is


72. The compound of claim 71, wherein n is 1 and R₂ is —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups.
 73. The compound of claim 71, wherein R₁ is —CF₃; n is 0; r is 1 and R₈ is -halo.
 74. The compound of claim 71, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; Ar² is r is 1 and R₈ is —CH₃.
 75. The compound of claim 71, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; Ar² is r is 1 and R₈ is -halo.
 76. The compound of claim 71, wherein R₁ is —CH₃; n is 0; Ar² is r is 1 and R₈ is -halo.
 77. The compound of claim 71, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; r is 1 and R₈ is —CF₃.
 78. The compound of claim 71, wherein R₁ is —CH₃; n is 0; r is 1 and R₈ is —CF₃.
 79. The compound of claim 71, wherein R₁ is —CF₃; n is 0; r is 1 and R₈ is —CF₃.
 80. The compound of claim 71, wherein R₁ is —F, —Cl, —Br, or —I; n is 0; r is 1 and R₈ is -tert-butyl.
 81. The compound of claim 71, wherein R₁ is —CF₃; n is 0; r is 1 and R₈ is -tert-butyl.
 82. The compound of claim 8, wherein Ar¹ is

and Ar² is


83. The compound of claim 82, wherein n is 1 and R₂ is —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, each of which is unsubstituted or substituted with one or more R₅ groups.
 84. The compound of claim 82, wherein R₁ is —F, —Cl, —Br, or —I; s is 1 and R₈ is -halo.
 85. The compound of claim 82, wherein R₁ is —CH₃; s is 1 and R₈ is -halo.
 86. The compound of claim 82, wherein R₁ is —CF₃; s is 1 and R₈ is -halo.
 87. The compound of claim 82, wherein R₁ is —F, —Cl, —Br, or —I; s is 1 and R₈ is —CH₃.
 88. The compound of claim 82, wherein R₁ is —CF₃; s is 1 and R₈ is —CH₃.
 89. The compound of claim 82, wherein R₁ is —F, —Cl, —Br, or —I; s is 1 and R₈ is —CF₃.
 90. The compound of claim 82, wherein R₁ is —CH₃; s is 1 and R₈ is —CF₃.
 91. The compound of claim 82, wherein R₁ is —CF₃; s is 1 and R₈ is —CF₃.
 92. The compound of claim 82, wherein R₁ is —F, —Cl, —Br, or —I; s is 1 and R₈ is —CH₂CF₃.
 93. The compound of claim 82, wherein R₁ is —CF₃; s is 1 and R₈ is —CH₂CF₃.
 94. The compound of claim 82, wherein R₁ is —F, —Cl, —Br, or —I; s is 1 and R₈ is -tert-butyl.
 95. The compound of claim 82, wherein R₁ is —CF₃, s is 1 and R₈ is -tert-butyl.
 96. The compound of claim 1, wherein m is
 0. 97. The compound of claim 1, wherein Ar¹ is a pyridyl group.
 98. The compound of claim 1, wherein Ar² is


99. The compound of claim 98, wherein s is 0 or
 1. 100. The compound of claim 1, wherein Ar² is


101. The compound of claim 100, wherein r is 0 or
 1. 102. The compound of claim 1, wherein Ar² is


103. The compound of claim 102, wherein each R₈ is independently —H, halo, —(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).
 104. The compound of claim 103, wherein s is 0, 1 or
 2. 105. A composition comprising the compound or a pharmaceutically acceptable salt of the compound of claim 1 and a pharmaceutically acceptable carrier or excipient.
 106. A method for treating pain in an animal, comprising administering to an animal in need thereof an effective amount of the compound or a pharmaceutically acceptable salt of the compound of claim
 1. 